JPH03218340A - Pantothenic acid derivative - Google Patents

Abstract

NEW MATERIAL:A compound expressed by formula I [R<1> and R<2> are H or OH protecting group; R<3> is 5-25C monovalent aliphatic hydrocarbon group or NR<4>R<5> (R<4> is 5-25C monovalent aliphatic hydrocarbon group; R<5> is H or monovalent aliphatic hydrocarbon); A is 2-16C bivalent aliphatic or bivalent aromatic hydrocarbon group or bivalent aromatic heterocycle group; either one of X and Y is NR<6> and the other is O, S or NR<7> (R<6> and R<7> are H or lower alkyl); (n) is 1-4]. EXAMPLE:N-[4-(Oleoyloxy)phenyl]-3-[N-2,2,5,5-tetramethyl-1,3-dioxane-4 -carbonyl) amino]propaneamide. USE:An acyl CoA-cholesterol acyl transferase inhibitor. A medicine having an action to lower lipid in blood and anti-arteriosclerosis action based on the inhibition of cholesterol absorption together. PREPARATION:For example, a compound expressed by formula II (R<11> and R<21> are OH protecting group) is subjected to a reaction with a compound expressed by the formula R<3>-COZ<1> (Z<1> is OH, halogen, etc.) or compound expressed by the formula R<4>-NCO to provide the compound expressed by formula I.

Description

DETAILED DESCRIPTION OF THE INVENTION Industrial Application Fields The present invention provides acyl CoA-cholesterol-acyltransferase (Acyl CoA-cholesterol-A
The present invention relates to a pantothenic acid derivative having excellent inhibitory activity against cyltransferase (hereinafter abbreviated as "ACAT").

<Prior art and problems> In recent years, in atherosclerosis, which is a common type of arteriosclerosis, fat deposits have been observed from the earliest stages of the onset of arteriosclerosis, and the main component of this accumulated fat is cholesterol; Furthermore, numerous histopathological and biochemical studies have revealed that this cholesterol is derived from plasma lipids.

Furthermore, various epidemiological studies have shown that hyperlipidemia is a major risk factor for arteriosclerotic diseases. Therefore, the treatment of hyperlipidemia has become increasingly important in terms of reducing the risk of arteriosclerotic disease, and therapeutic drugs for this purpose do not just lower serum lipid levels, but also improve serum lipid balance or improve arteriosclerotic disease. The emergence of a drug that can actively prevent the onset of sclerosis is desired.

A large number of drugs have already been provided for the treatment of hyperlipidemia, and although they have shown some clinical efficacy in lowering total serum cholesterol, they are not necessarily effective in reducing mortality due to arteriosclerotic diseases. Not sufficiently effective. In addition, in recent years, with the elucidation of the lipid metabolic system, drugs that control serum lipid levels have been developed, which are effective in increasing the serum level of high-density ribon protein (HDL) and decreasing the level of low-density ribon protein (LDL). or drugs that inhibit cholesterol biosynthesis and consequently reduce serum lipid levels (HMGCoA redu
ctase inhibitors) etc. are being developed. However, although these drugs are effective in improving blood lipid levels, they have little effect on controlling the absorption of dietary cholesterol from the intestinal wall, and furthermore, they may actively inhibit the onset or progression of arteriosclerosis. It has no preventive effect, and whether or not it can reduce the risk of arteriosclerotic disease must be examined in the future.

On the other hand, ACAT, known as an integral membrane enzyme, is present in large amounts in intracellular microsomes of the liver and small intestine, and controls the synthesis of cholesterol esters. Furthermore, the existence of two types of isozymes is currently known in this enzyme, but their structures and their physiological roles have not yet been elucidated because it is difficult to isolate and purify this enzyme. However, ACAT is involved in the absorption of cholesterol between the intestines and its accumulation as cholesterol ester in cells, and its activity is known to be enhanced in arteriosclerotic lesions. It is expected to be useful as a drug that has both a blood lipid-lowering effect based on absorption inhibition and an anti-arteriosclerotic effect.

Therefore, the present inventors conducted intensive research to synthesize a substance having excellent ACAT inhibitory activity, and as a result, they have now completed the present invention.

<Disclosure of the Invention> According to the present invention, in the following general formula, R1 and R2 are the same or different and each represents a hydrogen atom or a hydroxyl group protecting group; R3 is saturated or unsaturated, and linear or branched. C5-Cp optionally substituted with a chain or cyclic aromatic group
s Monovalent aliphatic hydrocarbon group, where R4 is saturated or unsaturated and linear, branched or cyclic C5-C
2S represents a monovalent aliphatic hydrocarbon group, and R5 is a hydrogen atom or a monovalent aliphatic hydrocarbon which is saturated or unsaturated and may be substituted with a linear, branched or cyclic aromatic group. Represents a group: A is saturated or unsaturated and optionally substituted with a linear, branched or cyclic aromatic group 02-CI6 divalent aliphatic hydrocarbon group, divalent aromatic hydrocarbon group or represents a divalent aromatic heterocyclic group; either one of X and Y represents 1N1 and R7 and the other represents 10-, -S1 or 1N, where R6
and R'l each represent a hydrogen atom or a lower alkyl group; n is an integer of 1 to 4. A compound represented by the following is provided.

In this specification, the term "lower" is used to indicate that the atomic group or compound modified with this term has 6 or less carbon atoms, preferably 4 or less carbon atoms.

Further, the "hydroxyl protecting group" can be any protecting group that can be removed by hydrolysis or hydrogenolysis, and examples thereof include those exemplified below. Methyl, methoxyethyl, methylthiomethyl, penzyloxymethyl, t-butoxymethyl, 2-methoxyethoxymethyl, 2,2.2-}lichloroethoxymethyl, bis(2chloroethoxy)methyl, 1-ethoxyethyl, 1- Methyl-1-methoxyethyl, 1-(isopropoxy)ethyl, 2,2.2-trichloroethyl, t
-butyl, allyl, cinnamyl, benzyl, pmethoxybenzyl, 0-nitrobenzyl, pnitrobenzyl, p
- Substituted or unsubstituted alkyl or alkenyl groups such as chlorobenzyl, O-chlorobenzyl, p-cyanobenzyl, diphenylmethyl, α-naphthyldiphenylmethyl, triphenylmethyl, di(p-methoxyphenyl)methyl; tetrahydropyranyl; tetrahydrothioviranyl,
Heterocyclic groups such as 4-methoxytetrahydropyranyl, 4-methoxytetrahydrothioviranyl, tetrahydrofuranyl, tetrahydrothiofuranyl; trimethylsilyl, triethylsilyl, isopropyldimethylsilyl, t
-Substituted silyl groups such as butyldimethylsilyl, t-butyldiphenylsilyl, methyldiisopropylsilyl, methyldit-butylsilyl, tribenzylsilyl, triphenylsilyl, triisopropylsilyl; formyl, acetyl, probionyl, chloroacetyl, dichloroacetyl, trichloro Acetyl, trifluoroacetyl, methoxyacetyl, triphenylmethoxyacetyl, phenoxyacetyl, p-chlorophenoxyacetyl, 2.6-
Dichloro-4-methylphenoxyacetyl, phenylacetyl, chlorodiphenylacetyl, 3-phenylpropionyl, 3-penzoylpropionyl, isobutyroyl, monosuccinoyl, 4-oxobentanoyl, bivaloyl, 2-butenoyl, (E)-2-methyl-2 -Butenoyl, benzoyl, 2-chlorobenzoyl, 3-nitrobenzoyl, 2-fluorobenzoyl, 3-trifluorobenzoyl, 3-trichlorobenzoyl, 4-phenylbenzoyl, 2I4,6-trimethylbenzoyl, α
- Acyl group such as naphthoyl; methoxycarbonyl, ethoxycarbonyl/L/, 2.2.2 - triethoxycarbonyl, isobutoxycarbonyl, vinyloxycarbonyl, aryloxycarbonyl, cinnamyloxycarbonyl, p-nitrophenoxy Cycarbonyl, penzyloxycarbonyl, p-methoxybenzyl9 Oxycarbonyl, 3,4-dimethoxybenzyloxycarbonyl, 0-nitrobenzyloxycarbonyl, p
- Substituted oxycarbonyl groups such as nitrobenzyloxycarbonyl; phenylcarbamoyl, naphthylcarbamoyl, toluylcarbamoyl, fluorophenylcarbamoyl, difluorophenylcarbamoyl, nitrophenylcarbamoyl, cyanophenylcarbamoyl, penzylcarbamoyl, methylcarbamoyl, ethylcarbamoyl, Isobrobylcarbamoyl, butylcarbamoyl, cyclohexylcarbamoyl, cycloprobylmethylrubamoyl, phenylthiocarbamoyl, naphthylthiocarbamoyl, toluylthiocarbamoyl, fluorophenylthiocarbamoyl, difluorophenylthiocarbamoyl, nitrophenylthiocarbamoyl, cyanophenyl Substituted carbamoyl groups such as thiocarbamoyl, pendylthiocarbamoyl, probylthiocarbamoyl, butylthiocarbamoyl, and the like.

In addition, in the above formula (1), when R1 and R2 represent a protecting group for a water 10 acid group, R1 and R2 are
methylene, ethylidene, 1,t-butylethylidene, 1-phenylethylidene, 2,2.2-MJ
Chloroethylidene, isopropylidene, butylidene, cyclobenzylidene, cyclohexylidene, cycloheptylidene, penzylidene, p-methoxybenzylidene, 2
, 4-dimethoxybenzylidene, p-dimethylaminobenzylidene, 〇-nitropenzylidene, methoxymethylene, ethoxymethylene, dimethoxymethylene, 1-methoxyethylidene, 1,2-dimethoxyethylidene, α-methoxybenzylidene, etc. You can also do that.

Examples of the "saturated or unsaturated linear, branched, or cyclic monovalent aliphatic hydrocarbon group" include the following.

(1) Alkyl group: For example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, pentyl, neopentyl, isopentyl, t-pentyl, ■-ethyl 11 lupentyl, 1-isopropylbentyl, 1- t-butylpentyl, 2-ethylpentyl, 2-isoprobylpentyl, 2-t-butylpentyl, 3-ethylpentyl,
3-isoprobylpentyl, 3-t-butylpentyl,
hexyl, 1-ethylhexyl, 1-isopropylhexyl, 1-tbutylhexyl, 2-ethylhexyl, 2
-isobrobylhexyl, 2-t-butylhexyl, 3
Ethylhexyl, 3-isopropylhexyl, 3-t-
butylhexyl, heptyl, ■-ethylheptyl, 1-
Isoprovirheptyl, 1-neopentylheptyl, 2
-Ethylheptyl, 2-isobrobylheptyl, 2-neopentylheptyl, 3-ethylheptyl, 3-isoprobylheptyl, 3-neopentylheptyl, octyl, 1-ethyloctyl, ■-isopropyloctyl, 1
-t-butyloctyl, 2-ethyloctyl, 3-isobrobyloctyl, 4-t-butyloctyl, nonyl, ■
-Methylnonyl, 1-ethylnonyl, 1-isopropylnonyl, ■-isobutylnonyl, 12 2-methylnonyl, 2-ethylnonyl, 3-isopropylnonyl, 4-isobutylnonyl, decyl, 1-ethyldecyl, 1.1-diethyldecyl, 1-t-Butyldecyl, 3-ethyldecyl, II3-diethyldecyl, 2-
t-butylundecyl, undecyl, 1-isopropylundecyl, 1.1-diethylundecyl, 2-isopropyllundecyl, 1.2-diethylundecyl, dodecyl, 1-t-butyldodecyl, 1-isobrobildodecyl, 1,1 diethyldodecyl, 2-t-butyldodecyl, 3-isoprobildodecyl, 2,4-diethyldodecyl, tridecyl, 1,1-diethyltridecyl, 1-t
-Butyltridecyl, 1,5-diethyltridecyl, 3
-t-butyltridecyl, tetradecyl, 1-isobutyltetradecyl, pentadecyl, 1-methylpentadecyl, 1,1-dimethylpentadecyl, 1-ethylpentadecyl, 1,1-diethylpentadecyl, 1-isopropylpentadecyl, 1-t-butylpentadecyl, 2
-isobutyltetradecyl, 3-methylpentadecyl,
2,6-di13 methylpentadecyl, 2-ethylpentadecyl, 1,4
-diethylpentadecyl, 3-isoprobylpentadecyl, 2-t-butylbentadecyl, hexadecyl, 1,
1-dimethylhexadecyl, 1methylhexadecyl, 1
-Ethylhexadecyl, 1-isopropylhexadecyl, 1-t-butylhexadecyl, 1,3-dimethylhexadecyl, 2methylhexadecyl, 4-ethylhexadecyl, 3-isopropylhexadecyl, 4-t- Butylhexadecyl, heptadecyl, 1-methylheptadecyl, 1,1-dimethylheptadecyl, 1-ethylheptadecyl, 1-isopropylheptadecyl, 1-t-butylheptadecyl, 2-methylheptadecyl, 3.5 -dimethylhebutadecyl, 2-ethylheptadecyl, 5-isopropylhebutadecyl, 3-t-butylheptadecyl,
Octadecyl, 1-methyloctadecyl, 1,1-dimethyloctadecyl, 1-ethyloctadecyl, 1,1-diethyloctadecyl, 2-methyloctadecyl, 2.3
1-dimethyloctadecyl, 5-ethyloctadecyl, 1
4 1.2-diethyl octadecyl, nonadecyl, 1-methylnonadecyl, 1,1-dimethylnonadecyl, 1-t-butylnonadecyl, 2-methylnonadecyl, 2,3-dimethylnonadecyl, 3-t-butylnonadecyl, icosyl, 1-methylicosyl , II1-dimethylicosyl, 1
-ethyl icosyl, 1t-butyl icosyl, 4-methyl icosyl, 2,2-dimethyl icosyl, 3-ethyl icosyl, 2t-butyl icosyl, etc.

(2) Alkenyl group: For example, vinyl, 1-bropenyl, ■-methyl-2-probenyl, 1-methyl-1-butenyl, 2-butenyl, 1-methyl-3-butenyl, 1-pentenyl, ■-methyl-2 −
Pentenyl, 1-ethyl-3bentenyl, 4-pentenyl, ■,3-pentadienyl, 2,4-pentadienyl, 1-hexenyl, 1-methyl-2-hexenyl, 3-
Hexenyl, 4-hexenyl, 1-butyl-5-hexenyl, 1,3-hexadienyl, 2,4-hexadienyl, 1-heptenyl, 2-heptenyl, 3-heptenyl 1
5-heptenyl, 4-hephtenyl, 5-heptenyl, 6-heptenyl, 1,3-hebutadienyl, 2I4-hebutadienyl,
1-octenyl, 2-octenyl, 3-octenyl, 4-
octenyl, 5-octenyl, 6-octenyl, 7-octenyl, 1-nonenyl, 2-nonenyl, 3-nonenyl, 4-nonenyl, 5-nonenyl, 6-nonenyl, 7-nonenyl, 8-nonenyl, 9-decenyl, 1-methyl-9
-decenyl, 1,1-dimethyl-9-decenyl, 1-ethyl-9-decenyl, 6-undecenyl, 1-methyl-
6-undecenyl, 1.1-dimethyl-6-undecenyl, 6-tridecenyl, 1-methyl-6-tridecenyl, 1.1-dimethyl-6-tridecenyl, 8-tridecenyl, 1-methyl-8-tridecenyl, 1, 1-dimethyl-8-tridecenyl, 10-tridecenyl, 1-methyl-10-tridecenyl, 1.1-dimethyl-1O-
tridecenyl, 10-pentadecenyl, 1-methyl-1
0-pentadecenyl, 1,1-dimethyl-10-pentadecenyl, 8-pentadecenyl, 1-methyl-8-pentadecenyl, 16 1,1-dimethyl-8-pentadecenyl, 12-hebutadecenyl, 1-methyl-12-heptadecenyl, ■、１
-dimethyl-12-heptadecenyl, 10-hebutadecenyl, 1-methyl-10-hebutadecenyl, 1,1-dimethyl-10-heptadecenyl, 8-hebutadecenyl,
1-Methyl-8-hebutadecenyl, 1,1-dimethyl-
8-heptadecenyl, ■-ethyl-8-heptadecenyl, 8.11-heptadecenyl, 1-methyl-8,l
1-hebutadecadienyl, 8,11.14-hebutadecatrienyl, and the like.

(3) Alkynyl group: e.g. probagyl, 2-butynyl, 1-methyl-3-butynyl, 2-pentynyl, aethyl-3-pentynyl, 1-
Isoprobyl-4-pentynyl, 13-pentadiynyl, 2,4-pentadiynyl, 1-hexynyl, 1-methyl-2-hexynyl, 2-methyl-3-hexynyl, 1-
Ethyl-4-hexynyl, 5-hexynyl, 1,3-hexadiynyl, 2,4-hexadiynyl, 1-heptynyl, 1-methyl-2-heptynyl, 3-heptynyl, 1
17 1-Ethyl-4-heptynyl, 2-propyl-5-heptynyl, 2-ethyl-6-heptynyl, 1,3-hebutadiynyl, 2,4-hebutadiynyl, 1-octynyl, 1-
Methyl-2-octynyl, 3methyl-1-octynyl,
4-methyl-1-octynyl, 1-methyl-5-octynyl, 6-methyl-1-octynyl, 7-octynyl,
1-nonynyl, 2-methyl-1-nonynyl, 3-methyl-1-nonynyl, 1-methyl-4-nonynyl, 5-nonynyl, 6-methyl-1-nonynyl, 1-methyl-7-nonynyl, 8-nonynyl, 9-decynyl, 1-methyl-9-decynyl, 1,1-dimethyl-9-decynyl, 1-ethyl-9-decynyl, 6-undecynyl, 1-methyl-6-
undecynyl, 1,1-dimethyl-6-undecynyl,
6-tridecynyl, 1-methyl-6-tridecynyl, 1
．． 1-dimethyl-6-tridecynyl, 8-tridecynyl, 1-methyl-8-tridecynyl, 1,1-dimethyl=
8-tridecynyl, 10-tridecynyl, 1-methyl-
10-tridecynyl, 1,1-dimethyl-1018 tridecynyl, 10-pentadecynyl, ■-methyl-1
0-pentadecynyl, ■,1-dimethyl-10-pentadecynyl, 8-pentadecynyl, 1-methyl8-pentadecynyl, 1,1-dimethyl-8-pentadecynyl, 1
2-heptadecinyl, 1-methyl-12-heptadecinyl, 1.1-dimethyl-12-heptadecinyl, 10-heptadecinyl, l-methyl-10-heptadecinyl, 1
, 1-dimethyl-10-heptadecinyl, 8-heptadecinyl, 1-methyl-8-heptadecinyl, 1,1-dimethyl-8-heptadecinyl, 1-ethyl-8-hebutadecinyl, 8,11-hebutadecadiynyl, 1-methyl- 8,11-heptadecadiynyl, 8.11.14-heptadecatriynyl, etc.

(4) Cycloalkyl group: for example, cyclopyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, barhydronaphthyl, etc.

(5) Cycloalkenyl group: For example, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentakienyl,
Cyclohexadienyl, cyclohebutadienyl, cyclooctadienyl, etc.

(6) Cycloalkylalkyl group: For example, cyclohexylmethyl, cyclopentylmethyl, (4-isopropylcyclohexyl)methyl, (4-t-butylcyclohexyl)methyl, (4-neopanthylcyclohexyl)methyl, 2-cyclopentylethyl, 2- Cyclohexylethyl, 3-cyclobentylpropyl, 3-cyclohexylpropyl, 1-cyclopentylpentyl, 1-cyclohexylpentyl, 1-cyclohexylmethylpentyl, 3-cyclopentylpentyl, 2-cyclohexylpentyl, 2-cyclohexylmethylpentyl, 1-
(4-t-butylcyclohexyl)methylpentyl, 1
-cyclobentylhexyl, -cyclohexylhexyl, 1-cyclopentylmethylhexyl, 2-cyclopentylhexyl, 2-cyclohexylhexyl, 3-cyclopentylmethylhexyl, 1-(4-neopentylcyclohexyl)methylhexyl, 1-cyclopentylheptyl , 1-cyclohexylmethylheptyl,
l-(4-isobrobylcyclohexyl)methylheptyl, 3-cyclopentylheptyl, 2-cyclohexylmethylheptyl, 4(4-isobrobylcyclohexyl)methylheptyl, l-cyclopentyloctyl, 1-
cyclohexyloctyl, ■-cyclopentylmethyloctyl, 2-cyclopentyloctyl, 3-cyclohexyloctyl, 2-cyclopentylmethyloctyl, 1
-cyclopentylnonyl, 1-cyclohexylnonyl,
1-cyclohexylmethylnonyl, 3-cyclobentylnonyl, 2-cyclohexylnonyl, 2-cyclohexylmethylnonyl, l-cyclopentyldecyl, ■-cyclopentylundecyl, 1-cyclohexylundecyl, 1cyclopentyldodecyl, 1- Cyclopentyltridecyl, 2-cyclopentyldecyl, 3-cyclopentylundecyl, 3-cyclohexylundecyl, 2-cyclopentyldodecyl, 2-cyclopentyltridecyl, 1-cyclopentyltetradecyl, 1-cyclohexyltetradecyl, 2-cyclopentyl Tetradecyl, 3-cyclohexyltetradecyl, etc.

(7) Cycloalkenylalkyl group: e.g. 2-cyclohexen-1-ylmethyl, ■-cyclopentene-
1-ylmethyl, 2-(2-cyclopenten-1-yl)ethyl, 2-(1-cyclohexen-1-yl)
Ethyl, 3-(1-cyclopenten-1-yl)propyl, 3-(1-cyclohexen-1-yl)propyl, 4-(1-cyclohexen-1-yl)butyl, 1
-(1-cyclobenten-1-yl)pentyl, 5-(
1-cyclobenten-1-yl)bentyl, 1-1(cyclohexen-1-yl)pentyl, 5(1-cyclohexen-1-yl)pentyl, 1(1-cyclohexen-1-ylmethyl)pentyl, 1-( 1-cyclopenten-1-yl)hexyl, 6-(1-cyclopenten-1-yl)hexyl, 1-(1-cyclohexene-1
-yl) 22 hexyl, 6-(1-cyclohexen-1-yl)hexyl, 1-(2-cyclopenten-1-ylmethyl)hexyl, 1-(1-cyclopenten-1-yl)heptyl, 7-(1-cyclopentene) =1-yl)heptyl,
1-(1-cyclohexen-1-ylmethyl)heptyl, 1-(1-cyclopenten-1-yl)octyl, 1
-(2-cyclobenten-1-yl)octyl, 1-(
2cyclohexen-1-yl)octyl, 8-(2cyclohexen-1-yl)octyl, 1(1-cyclopenten-1-ylmethyl)octyl, 1-(1-cyclopenten-1-yl)nonyl, 9-(1-cyclopenten-1-yl)nonyl, 1-(1-cyclohexene-1-
yl)nonyl, 9-(1-cyclohexen-1-yl)nonyl, 1-(1-cyclohexen-1-ylmethyl)nonyl, 1-(1-cyclopenten-1-yl)
Decyl, 10-(1-cyclopenten-1-yl)decyl, 1-(2-cyclobenten-1-yl)undecyl, 1-(2-cyclohexen-1-yl)undecyl, 1-(1-cyclopentene) -1il)
dodecyl, 1-(1-cyclobenten-1-yl)tridecyl, 1-(2-cyclobenten-1-yl)tetradecyl, 1-(3-cyclohexen-1-yl)tetradecyl, and the like.

(8) Alkylcycloalkyl group and alkenylcycloalkyl group: e.g. 1-methylcyclobutyl, 2-ethylcyclobutyl, 2
-propylcyclobutyl, ■-butylcyclobutyl, 1
-pentylcyclobutyl, 1-hexylcyclobutyl,
1-heptylcyclobutyl, 1-octylcyclobutyl, 1-nonylcyclobutyl, 2-pentylcyclobutyl, 2-hexylcyclobutyl, 2-heptylcyclobutyl, 2-octylcyclobutyl, 2-nonylcyclobutyl , 1-decylcyclobutyl, 1-undecylcyclobutyl, ■-dodecylcyclobutyl, 1-pentadecylcyclobutyl, 1-(9-octadecenyl)cyclobutyl, 1-methylcyclopentyl, 2methylcyclopentyl, ■-ethylcyclopentyl 24, 1-propylcyclopentyl, 1-butylcyclopentyl, 2-butylcyclopentyl, 1bentylcyclopentyl, ■-hexylcyclopentyl, 3-hexylcyclopentyl, 1-heptylcyclopentyl, 1-octylcyclopentyl, 2-octylcyclobentyl,
1-decylcyclopentyl, 1-dodecylcyclopentyl, ■-tridecylcyclopentyl, l-tetradecylcyclopentyl, 1-(9-octadecenyl)cyclopentyl, ■-methylcyclohexyl, 1-ethylcyclohexyl, 1-propylcyclohexyl, 2-methylcyclohexyl , 3-ethylcyclohexyl, 4-propylcyclohexyl, 1-butylcyclohexyl, 1-bentylcyclohexyl, 1-hexylcyclohexyl, 4
-butylcyclohexyl, 4-pentylcyclohexyl, 4-hexylcyclohexyl, 1-heptylcyclohexyl, 1-octylcyclohexyl, 1-nonylcyclohexyl, 1-undecylcyclohexyl, l-hexadecylcyclohexyl, 125 (9-octadecenyl) such as cyclohexyl.

(9) Alkylcycloalkenyl group and alkenylcycloalkenyl group: for example, 1-methyl-2-cyclopentenyl, 1-ethyl-2-cyclobentenyl, 1-propyl-2-cyclopentenyl, 1-butyl-2-cyclopentenyl, -Pentyl-2-cyclopentenyl, 1-hexyl-2-cyclopentenyl, 1-heptyl-2-cyclopentenyl, 1-octyl-2-cyclobentenyl, 2-methyl-2-cyclopentenyl, 3-ethyl-2 -cyclopentenyl, 2-propyl-3-cyclopentenyl, 3-butyl-2-cyclopentenyl, 2-pentyl-2-cyclopentenyl, 3-
hexyl-3-cyclopentenyl, 2-heptyl-2-
Cyclopentenyl, 2-octyl-3-cyclopentenyl, 1-decyl-2-cyclopentenyl, 1-dodecyl-2-cyclopentenyl, 1-tridecyl-2-cyclopentenyl, 1-tetradecyl-2-cyclopentenyl,
1-(9-octadecenyl)-2-cyclo26 lobentenyl, I-methyl-2-cyclohexenyl, 1
-ethyl-2-cyclohexenyl, 1-proyl-2-
Cyclohexenyl, 1-butyl-2-cyclohexenyl, 1-pentyl-2-cyclohexenyl, ■-hexyl-2-cyclohexenyl, 1-heptyl-2-cyclohexenyl, 4-methyl-2-cyclohexenyl, 2 -Ethyl 2-cyclohexenyl, 3-propyl-2-cyclohexenyl, 4-butyl-3-cyclohexenyl, 3-
Pentyl-3-cyclohexenyl, 4-hexyl-3-cyclohexenyl, 4-heptyl-3-cyclohexenyl,
1-octyl-2-cyclohexenyl, ■-nonyl-2
~cyclohexenyl, 1-undecyl-2-cyclohexenyl, 1-hexadecyl-2-cyclohexenyl, 1
(9-octadecenyl)-2-cyclohexenyl and the like.

Examples of the "aromatic group" in "a saturated or unsaturated linear or branched monovalent aliphatic hydrocarbon group substituted with a cyclic aromatic group" include, for example, 27 phenyl, naphthyl and aromatic heterocyclic groups such as furyl, chenyl, pyridyl, quinolyl, isoquinolyl, pyridazinyl, pyrazinyl, indolyl, benzoxadiazolyl, imidazolyl, benzothiadiazolyl, triazolyl, and tetrazolyl. I can do it. This aromatic group may be substituted, for example, a halogen atom such as a chlorine atom, a bromine atom, a fluorine atom, a lower alkyl group, a lower alkoxy group, a cyano group, a nitro group, a trichloromethyl group, a trifluoromethyl group. ,
Examples of substituents include hydroxy group, phenyl group, phenoxy group, and lower alkylthio group.

In the above general 2, the saturated or unsaturated linear, branched or cyclic monovalent aliphatic hydrocarbon group represented by R3 or R4 includes relatively long chain ones among the above, That is, those having 5 to 25 carbon atoms, preferably 8 to 22 carbon atoms, are used, while saturated or unsaturated, linear, branched, or cyclic monovalent carbon atoms, which can be represented by R5, are used. The aliphatic hydrocarbon group may be either short-chain or long-chain, but generally it is relatively short-chain, preferably having 1 to 10 carbon atoms, more preferably 1 to 8 carbon atoms. Are suitable.

Therefore, in the general formula (1), R3 may be replaced by, for example,
2-cyclopentylethylamino, 2-cyclohexylethylamino, 3-cyclobentylbropylamino, 3-
Cyclohexylpropylamino, 2-cyclopentyl-1-methylethylamino, 2-cyclobentyl-1.1
-dimethylethylamino, 2-cyclohexyl-1-methylethylamino, 3-cyclopentylbropylamino, 3-cyclohexylpropylamino, 4-cyclohexyl-1.1-dimethylbutylamino, 1-methylbentylamino , 1.1-dimethylpentylamino, 1-
Ethylpentylamino, 1-cyclohexyl-4-methylbentylamino, ■-cyclobentylamino-4-methylpentylamino, 2-methy29 lupentylamino, 1,2-dimethylpentylamino,
2-ethylpentylamino, 2-cyclohexyl-4-
Methylpentylamino, 2-cyclopentyl-4-methylpentylamino, 3-methylpentylamino, 1.3
-dimethylbentylamino, 3-ethylpentylamino, 1-hexyl 3-methylpentylamino, 1-
Cyclopentyl-3-methylpentylamino, hexylamino, 1-methylhexylamino, II1-dimethylhexylamino, 1-ethylhexylamino, 1,1
diethylhexylamino, ■-probylhexylamino, 1-butylhexylamino, 1-cyclopentylhexylamino, 2-methylhexylamino, l,2-dimethylhexylamino, 2-ethylhexylamino, 1,
2-diethylhexylamino, 2-probylhexylamino, 2-butylhexylamino, 6-cyclobentyhexylamino, 6-cyclohexylhexylamino,
Heptylamino, l-ethylheptylamino, 1.1
-dimethylheptylamino, 1 to cyclohexylhep3
0 thylamino, 1-cyclopentylheptylamino, 1-
Cyclohexylmethylheptylamino, 1 cyclopentylmethylheptylamino, octylamino, 1,1-dimethyloctylamino, 1-methyloctylamino, 1
-ethyloctylamino, 1,1-diethyloctylamino, 1-propyloctylamino, l-butyloctylamino, lcyclopentyloctylamino, ■-cyclohexyloctylamino, 1-cyclopentylmethyloctylamino, 1-cyclohexylmethyl octylamino, nonylamino, 1-methylnonylamino, 1,1
-dimethylnonylamino, ■1-ethylnonylamino, 1
, 1-diethylnonylamino, decylamino, 1-methyldecylamino, 1,1-dimethyldecylamino, 1
-ethyldecylamino, 1,1-diethyldecylamino, 1-cyclobentydecylamino, 1-cyclohexyldecylamino, 1-cyclobentylmethyldecylamino, 1-cyclohexylmethyldecylamino, undecyl Amino, 1-methylundecylamino, 1.1-31 dimethylundecylamino, dodecylamino, 1-methyldodecylamino, 1.1-dimethyldodecylamino, tetradecylamino, l-methyltetradecylamino, 1
, 1-dimethyltetradecylamino, pentadecylamino, ■-methylpentadecylamino, 1,1-dimethylpentadecylamino, hexadecylamino, l-methylhexadecylamino, 1,1-dimethylhexadecylamino, heptadecyl Amino, 1-methylheptadecylamino, 1.1-dimethylheptadecylamino, octadecylamino, 1-methyloctadecylamino, 1,
1 dimethyloctadecylamino, 3-cyclopentyl-2-propenylamino, 3-cyclohexy71z-2-
7” Lopenylamino, 1,1-dimethyl-3-butenylamino, 1-ethyl-3-butenylamino, 1-cyclopropyl-3-butenylamino, 1-methyl-2-pentenylamino, 1,1-dimethyl-2-pentenylamino , 1-ethyl-2-pentenylamino, 1-cyclopropyl-2-pentenylamino, 2-hexenylamino, 1-methyl-2-hexenylamino, 1.1-dimethyl2-
hexenylamino, 3-hexenylamino, ■-methyl-3-hexenylamino, 1,1-dimethyl-3-hexenylamino, 2-heptenylamino, 1-methyl-2
-heptenylamino, 2-octenylamino, 1-methyl-2-octenylamino, 3-nonenylamino, 1-methyl-3-nonenylamino, 1,1-dimethyl-3-nonenylamino, 1-ethyl-3-nonenylamino, 1-propyl -3-nonenylamino, 8-nonenylamino, 1-
Methyl-8-nonenylamino, Lldimethyl-8-nonenylamino, 1-ethyl-8nonenylamino, 9-decenylamino, 1-methyl-9-decenylamino, 1,1
-dimethyl-9=decenylamine, 1-ethyl-9-decenylamino, 6-undecenylamino, 1-methyl-
6=undecenylamino, 1,1-dimethyl-6-undecenylamino, 6-tridecenylamino, 1-methyl-6-tridecenylamino, 1,1-dimethyl-6
-tridecenylamino, 8-tridecenylamino, 1-methyl-8-tridecenylamino, 1.
1-dimethyl-8-tridecenylamino, 10-tridecenylamino, 1-methyl-10-tridecenylamino, 1.1-dimethyl-10-tridecenylamino, 1
0-pentadecenylamino, 1-methyl=10-pentadecenylamino, ■,1-dimethyl-10-hentadecenylamino, 8-pentadecenylamino, 1-methyl-
8-pentadecenylamino, 1,1-dimethyl-8-pentadecenylamino, 12-hebutadecenylamino, 1
-Methyl-12-hebutadecenylamino, 1,1-dimethyl-12-hebutadecenylamino, IO-heptadecenylamino, lmethyl-1O-hebutadecenylamino,
II1-dimethyl-10-hebutadecenylamino, 8-
Hebutadecenylamino, 1-methyl-8-hebutadecenylamino, 1,1-dimethyl-8-heptadecenylamino, 1-ethyl-8-hebutadecenylamino, 8.11
-hebutadecadienylamino, 1-methyl-8.11-
hebutadecagenylamino, 8,IL14-hebutadecatrienylamino, ■-ethylcyclobutylamino, 1-propylcyclobutylamino, 1-butylcyclobutylamino, 1-pentylcyclobutylamino, 1-hexylcyclobutylamino, 1-pentylcyclobutylamino, 1-octylcyclobutylamino, 1-nonylcyclobutylamino, 1-decylcyclobutylamino, 1-undecylcyclobutylamino, 1-
Dodecylcyclobutylamino, 1-pentadecylcyclobutylamino, 1-(9-octadecenyl)cyclobutylamino, 1-methylcyclobentylamino, 1-ethylcyclopentylamino, 1-propylcyclopentylamino, 1-butylcyclopentylamino , 1-hexylcyclopentylamino, 1-octylcyclopentylamino, 1-decylcyclopentylamino, 1-dodecylcyclopentylamino, 1-tridecylcyclopentylamino, 1-tetradecylcyclopentylamino, 1
(9-octadecenyl)cyclopentylamino, cyclohexylamino, 1-methylcyclohexylamino, 1
-propylcyclohexylamino, 35 1-pentylcyclohexylamino, 1-heptylcyclohexylamino, 1-nonylcyclohexylamino,
Monosubstituted amino groups such as 1-undecylcyclohexylamino, 1-hexadecylcyclohexylamino, 1(9-octadecenyl)cyclohexylamino; (2-cyclopentylethyl)ethylamino, (2-cyclobentylbutyl)ethylamino, ( 2-cyclopentylethyl)octylamino, (2-cyclohexylethyl)propylamino, (2-cyclohexylethyl)
Pentylamino, (2-cyclohexylethyl)decylamino, (3-cyclopentylpropyl)hexylamino, (3-cyclohexylpropyl)octylamino,
(2-Cyclopentyl-1-methylethyl)butylamino, (2-cyclobentyl-1,1-dimethylethyl)hexylamino, (2-cyclohexyl-1-methylethyl)decylamino, (3-cyclobentylpropyl)heptylamino , (3cyclohexylbropyl)octylamino, (436 cyclohexyl-Ll-dimethylbutyl)pentylamino, hexyl(1-methylbentyl)amino, (1.1
-dimethylpentyl)heptylamino, (1-ethylbentyl)decylamino, (1-cyclohexyl-4-methylpentyl)butylamino, (1-cyclopentyl-4-methylpentyl)bentylamino, (2-methylpentyl)decylamino, (1,2-dimethylpentyl)
Heptylamino, (2-ethylbentyl)dodecylamino, (2-cyclohexyl-4-methylpentyl)butylamino, (2-cyclopentyl-4-methylpentyl)probylamino, (3-methylbentyl)octylamino, ( 1.3-dimethylbentyl)heptylamino,
(3-ethylpentyl)nonylamino, (1-cyclohexyl-3-methylbentyl)butylamino, (1-cyclopentyl-3-methylbentyl)propylamino,
Dihexylamino, butylhexylamino, hexyloctylamino, decylhexylamino, (1-methylhexyl)pentylamino, (1,1-dime37thylhexyl)decylamino, (1-ethylhexyl)
undecylamino, (Ll-diethylhexyl)octylamino, heptyl(1-propylhexyl)amino,
(1-Butylhexyl)propylamino, (1-cyclobentylhexyl)butylamino, (2-methylhexyl)octylamino, decyl(1l2-dimethylhexyl)amino, (2-ethylhexyl)tetradecylamino, (1,2- diethylhexyl) octylamino, (
2-propylhexyl)dodecylamino, (2butylhexyl)octylamino, (6-cyclopentylhexyl)butylamino, (6-cyclohexylhexyl)propylamino, diheptylamino, (1-ethylheptyl)tridecylamino, (1. 1-dimethylhebutyl)
Pentylamino, (1-cyclohexylheptyl)pentylamino, (1-cyclopentylheptyl)hexylamino, (1-cyclohexylmethylheptyl)butylamino, (1-cyclopentylmethylheptyl)propylamino, octylpropylamino, 38 hexyl octyl Amino, (1,1-dimethyloctyl)bentylamino, hexyl(1-methyloctyl)amino, (1-ethyloctyl)pentylamino, (1,
■-diethyloctyl) butylamino, octyl (1-
propyloctyl)amino, (1-butyloctyl)hexylamino, (1-cyclopentyloctyl)bentylamino, (l-cyclohexyloctyl)butylamino,
(1cyclobentylmethyloctyl)propylamino,
(1-hexylmethyloctyl)propylamino, nonylpropylamino, (1-methylnonyl)heptylamino, (1,1-dimethylnonyl)hexylamino, (1-ethylnonyl)butylamino, (1,1-diethylnonyl) probylamino, hexyldecylamino,
(1-Methyldecyl)bentylamino, (1,1-dimethyldecyl)hexylamino, (1-ethyldecyl)butylamino, (1,1-diethyldecyl)bentylamino, (l-cyclopentyldecyl)butylamino, (
1-cyclohexyldecyl)propylamino, 39 (1-cyclopentylmethyldecyl)ethylamino, (
1-cyclohexylmethyldecyl) methylamino, butylundecylamino, (1-methylundecyl)propylamino, (1.1-dimethylundecyl)propylamino, butyldodecylamino, (l-methyldodecyl)
Propylamino, (1,1-dimethyldodecyl)propylamino, probyltetradecylamino, (1-methyltetradecyl)butylamino, (1,1-dimethyltetradecyl)propylamino, butylbentadecyl amino, (1- methylbentadecyl)butylamino, (1,1
-dimethylpentadecyl)propylamino, ethylhexadecylamino, ethyl(1-methylhexadecyl)amino, (1,1-dimethylhexadecyl)methylamino, hebutadecylmethylamino, (1-methylheptadecyl)methylamino , (1,1-dimethylheptadecyl)
Methylamino, methyloctadecylamino, ethyl (1
-methyloctadecyl)amino, ethyl(1,1-dimethyloctadecyl)amino, (3-cyclobentyl40 2-propenyl)hexylamino, (3-cyclohexyl-2-probenyl)heptylamino, (1,1-dimethyl-3- butenyl)octylamino, (1-ethyl-3-butenyl)nonylamino, (1-cyclopropyl-3-butenyl)decylamino, (1-methyl-2-pentenyl)decylamino, (1.1-dimethyl-2-pentenyl) ) nonylamino, (1-ethyl-2-pentenyl)decylamino, (1-cyclopropyl-2-pentenyl)heptylamino, (2-hexenyl)octylamino, (1-methyl-2-hexenyl)pentylamino, (1,1-dimethyl-2-hexenyl)decylamino, (3-hexenyl)butylamino, (1-methyl-3
-hexenyl)octenylamino, (1,■-dimethyl-3-hexenyl)octenylamino, di(2-heptenyl)amino, (1methyl-2-heptenyl)heptylamino, bentyl(2-octenyl) Amino, (1-methyl 2-octenyl)hexylamino, heptyl (3-
nonenyl)amino, (1-methyl-3-nonenyl)hexylamino, (1,1-dimethyl-3-nonenyl)hexylamino, (1-ethyl-3-nonenyl)pentylamino, butyl (1-propyl- 3-nonenyl)amino, (8-nonenyl)pentylamino, (1-
Methyl-8-nonenyl)bentylamino, (1,1-dimethyl-8-nonenyl)butylamino, (1-ethyl-
8-nonenyl)pentylamino, (9-decenyl)propylamino, (1-methyl-9-decenyl)pentylamino, (Ll-dimethyl-9-decenyl)butylamino, (1-ethyl-9-decenyl)propylamino, Pentyl(6-undecenyl)amino, (1-methyl-6-
undecenyl)butylamino, (1,1-dimethyl-6
-undecenyl)propylamino, pentyl(6-tridecenyl)amino, (1-methyl-6-tridecenyl)
Pentylamino, (1,1-dimethyl-6-tridecenyl)ethylamino, butyl(8-tridecenyl)amino, butyl(1-methyl-8-tridecenyl)amino, (
1,1-dimethyl-8-tridecenyl)ethyl a42 mino, ethyl(10-tridecenyl)amino, butyl(
1-methyl-10-tridecenyl)amino, (1,1-
Dimethyl-10-tridecenyl)propylamino, butyl(10-pentadecenyl)amino, butyl(1-methyl-10-pentadecenyl)amino, (L.1-dimethyl-10-pentadecenyl)propylamino, (8-
pentadecenyl)propylamino, (1-methyl-8-
pentadecenyl)propylamino, ethyl(1,1-dimethyl-8-pentadecenyl)amino, butyl(12-
hebutadecenyl)amino, ethyl(1-methyl-12-
hebutadecenyl)amino, (1,1-dimethyl-12-
heptadecenyl)propylamino, ethyl(10-hebutadecenyl)amino, (1-methyl-10-hebutadecenyl)propylamino, ethyl(1,1-dimethyl-1
0-hebutadecenyl)amino, (8-hebutadecenyl)
Methylamino, methyl(I-methyl8-hebutadecenyl)amino, ethyl(1.1dimethyl-8-hebutadecenyl)amino, (1ethyl-8-heptadecenyl)propylamino, 43 (8.11-heptadecadienyl) ) methylamino, methyl(1-methyl-8,1l-hebutadecadienyl)amino, methyl(8,IL14-hebutadecatrienyl)amino, (1-ethylcyclobutyl)pentylamino, heptyl(1-propylcyclobutyl) ) amino, (1
-butylcyclobutyl)hexylamino,butyl(1-
pentylcyclobutyl)amino, (1-hexylcyclobutyl)heptylamino, proyl(1-pentylcyclobutyl)amino, ethyl(1-octylcyclobutyl)amino, proyl(1-nonylcyclobutyl)amino, ethyl(1-pentylcyclobutyl)amino, -decylbutyl)amino,methyl(
1-undecylcyclobutyl)amino, (1dodecylcyclobutyl)methylamino, ethyl(1-pentadecylcyclobutyl)amino, methyl(1-(9-octadecenyl)cyclobutyl}amino, methyl(1-methylcyclopentyl)amino , (1-ethylcyclobentyl)probylamino, probyl(1-propylcyclopentyl)amino, (1-butylcyclopentyl)pentyl44 amino, (1-hexylcyclobentyl)methylamino, methyl(1-octylcyclopentyl) Amino, (1
-decylcyclopentyl)methylamino, (1-dodecylcyclopentyl)methylamino, methyl(1-tridecylcyclobentyl)amino, methyl(1-tetradecylcyclopentyl)amino, methyl {1-(9-octadecenyl) cyclopentyl}amino, cyclohexyloctylamino, beptyl (1-methylcyclohexyl)
Amino, hexyl (1-propylcyclohexyl) amino, hexyl (1-pentylcyclohexyl) amino,
(1-heptylcyclohexyl)bentylamino, butyl(1-nonylcyclohexyl)amino, ethyl(1-
undecylcyclohexyl)amino, ethyl(1-hexadecylcyclohexyl)amino, methyl(1-(9-
octadecenyl)cyclohexyl)amino, penzylhexylamino, penzylheptylamino, penzyloctylamino, penzyldecylamino, penzylnonylamino, penzylundecylamino, nonyl(245 phenylethyl)amino, nonyl(4-phenylbutyl) ) amino, 4-neobentylbenzylnonylamino, 4
-isopropylbenzylnonylamino, heptyl (4-
Examples include di-substituted amino groups such as neopentylbenzyl)amino.

Furthermore, examples of the "saturated or unsaturated linear, branched or cyclic divalent aliphatic hydrocarbon group" include those exemplified below.

(1) Alkylene groups and cycloalkylalkylene groups, such as ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene, hebutamethylene,
Octamethylene, nonamethylene, decamethylene, propylene, ethylethylene, isopropylethylene, probylethylene, butylethylene, isobutylethylene, cyclopentylethylene, cyclohexylethylene, cycloheptylethylene, 1.1-dimethylethylene, 1-
Methyltrimethylene, 2-methyltrimethylene, 1-ethyltrimethylene, 1-isopropyltrimethylene, ■
-isobutyltrimethylene, l-cyclo46 pentyltrimethylene, 1-cyclohexyltrimethylene, 2-isopropyltrimethylene, 2-isobutyltrimethylene, 2-cyclohexyltrimethylene, 1-methyltetramethylene, 1-isobutyltrimethylene Hexyltetramethylene, 1-isobutyltetramethylene, 1-cyclopentyltetramethylene, 1-cyclohexyltetramethylene,
2-methyltetramethylene, 2-isoprobyltetramethylene, 2-isobutyltetramethylene, 2-cyclopentyltetramethylene, 2-cyclohexyltetramethylene, 1-methylpentamethylene, 1-ethylpentamethylene, 1-isopropylbentamethylene, 1 -isobutylpentamethylene, 1cyclopentylpentamethylene,
1-hexylpentamethylene, 2-methylpentamethylene, 2-ethylpentamethylene, 2-isoprobylpentamethylene, 2-isobutylpentamethylene, 2
-Cyclopentylpentamethylene, 2-cyclohexylpentamethylene, methylpentamethylene, 3-ethylbentamethylene, 3-isoprobilpe47 , 1-ethylhexamethylene, 1-isopropylhexamethylene, 1-
Isobutylhexamethylene, 1-cyclopentylhexamethylene, 1-cyclohexylhexamethylene, 2-methylhexamethylene, 2-ethylhexamethylene, 2-
Isoprobylhexamethylene, 2-isobutylhexamethylene, 2-cyclopentylhexamethylene, 2-cyclohexylhexamethylene, 3-methylhexamethylene, 3-ethylhexamethylene, 3isoprobylhexamethylene, 3-isobutylhexamethylene, 3 -Cyclopentylhexamethylene, 3-cyclohexylhexamethylene, 1-methylhexamethylene, 1-ethylhbutamethylene, 1-isobutylhexamethylene, 1-isobutylhexamethylene, 1-cyclopentylhexamethylene, 1-cyclohexyl Butamethylene, 2-methylhebutamethylene, 2-ethylhebutamethylene, 2-isoprobylheptamethylene, 2-isobutylhebutamethylene, 2-cyclopentylhebutamethylene, 2-cyclohexylhebutamethylene, 3-methylhebutamethylene, 3- Ethyl heptamethylene, 3-isopropyl heptamethylene, 3-isobutyl heptamethylene,
3-Cyclopentylhebutamethylene, 3-cyclohexylhbutamethylene, 1-methyloctamethylene, 1-ethyloctamethylene, 1-isopropyloctamethylene, 1-isobutyloctamethylene, 1-cyclopentyloctamethylene, 1-cyclohexylocta methylene,
2-methyloctamethylene, 2ethyloccumethylene,
2-isopropyloctamethylene, 2-isobutyloctamethylene, 2-cyclopentyloctamethylene, 2-
Cyclohexyloctamethylene, 3-methyloctamethylene, 3-ethyloctamethylene, 3-isopropylctamethylene, 3-isobutyloctamethylene, 3-cyclopentyloctamethylene, 3-cyclohexyloctamethylene, 1-methylnoname49 Tylene, 1 -Ethylnonamethylene, 1-isoprobylnonamethylene, 1-isobutylnonamethylene, 1-cyclopentylnonamethylene, ■-Cyclohexylnonamethylene, 2-methylnonamethylene, 2-ethylnonamethylene, 2-isoprobylnonamethylene, 2 -isobutylnonamethylene, 2-cyclobentylinonamethylene, 2-cyclohexylnonamethylene, 3-methylnonamethylene, 3
-Ethylnonamethylene, 3-isoprobylnonamethylene, 3-isobutylnonamethylene, 3-cyclopentylnonamethylene, 3-cyclohexylnonamethylene, 1-methyldecamethylene, 1-ethylnodecethylene, 1-isoprobyldecamethylene , 1-isobutyldecamethylene,
1-Cyclopentyldecamethylene, l-cyclohexyldecamethylene, 2-methyldecamethylene, 2-ethyldecamethylene, 2-isopropyldecamethylene, 2-isobutyldecamethylene, 2-cyclopentyldecamethylene, 2-cyclohexyldecamethylene, 3 -02~CI6 alkylene groups such as methyldecamethylene, 3-ethyldecamethylene, 350 isoprobildecamethylene, 3-isobutyldecamethylene, 3-cyclopentyldecamethylene, 3-cyclohexyldecamethylene, and C,~C7 cycloalkyl02~ C. alkylene group.

(2) Cycloalkylene group: For example, 1,2-cyclobentylene, ■,3-cyclopentylene, II2-cyclohexylene, 1,3-cyclohexylene, 1.4
-cyclohexylene, 1,2-cycloheptylene, 1,
C, to C8 cycloalkylene groups such as 3-cycloheptylene and 1,4-cycloheptylene.

(3) Alkenylene group and alkynylene group: e.g. 2-
Butenylene, 1-methyl-2-butenylene, 1-ethyl-2-butenylene, 1-propylbutenylene, ■-butylbutenylene, 2-butynylene, 2-pentenylene, 2
- C451 to CIO alkenylene groups such as pentynylene, 2-hexenylene, 3-hexenylene, 2-hexynylene, 3-hexynylene, 2-heptenylene, 3-heptenylene, 2-heptynylene, 3-heptynylene, 2-octenylene, 4-octenylene, etc. and 04-C1. Alkynylene group.

(4) Cycloalkylene alkylene group: For example, 1.
1-pentamethylene ethylene, ■, 1-tetramethylene ethylene, 1,1-hexamethylene ethylene, 11-tetramethylene trimethylene, 1,1-pentamethylene trimethylene, 1.2-}rimethylene trimethylene, 1, 2-tetramethylene trimethylene, 1.1-}rimethylenepentamethylene, 1,1-tetramethylenebentamethylene, 1,1-bentamethylenepentamethylene, L2-}rimethylenepentamethylene, 1,2-
Tetramethylenebentamethylene, 1,2-pentamethylenepentamethylene, L3-}rimethylenebentamethylene, 1.1-}rimethylenehexamethylene, 1,
1-tetramethylenehexamethylene, 1,1-pentamethylenehexamethylene, 1.2-}limethylenehexamethylene, 1.2-tetramethylenehexamethylene, 1
, 2-pentamethylene hexamethylene, 1l3-trimethylene hexamethylene, 1.1-}rimethylene hexamethylene, ■,52 1-tetramethylene hexamethylene, 1.1-pentamethylene hexamethylene, 1.2-}rimethylene hexamethylene , ■, 2-tetramethylene to butamethylene, 1,
2-pentamethylene heptamethylene, 1.3-trimethylene heptamethylene, 1.1-}rimethylene octamethylene, 1.1-tetramethylene octamethylene, 1,1
-Pentamethyleneoctamethylene, L2-}rimethyleneoctamethylene, 1.2-tetramethyleneoctamethylene, 1.2-pentamethyleneoctamethylene, 1
．． 3-}rimethyleneoctamethylene, Ll-}rimethylenenonamethylene, 1.1-tetramethylenenonamethylene, ■,1pentamethylenenonamethylene, L2-trimethylenenonamethylene, 1.2-tetramethylenenonamethylene, 1 .2-pentamethylenenonamethylene, 1,
3-trimethylenenonamethylene, 1,1-trimethylenedecamethylene, 1,l-tetramethylenedecamethylene, II1-pentamethylenedecamethylene, 1,2-trimethylenedecamethylene, 1,2-tetramethylenedecamethylene, 04 such as 1.3-pentamethylene decamethylene 53 tyrene, 1.3-}rimethylene decamethylene
~C8 cycloalkylene-C, ~C, alkylene group.

The above-mentioned divalent aliphatic hydrocarbon groups may further include aromatic groups such as aryl groups such as phenyl and naphthyl; furyl,
Examples of divalent aliphatic hydrocarbon groups so substituted may be substituted with heteroaryl groups such as chenyl, pyridyl, indolyl, etc., such as phenylethylene, naphthylethylene, furylethylene, chenylethylene,
Examples include pyridylethylene, benzylethylene, naphthylmethylethylene, furylmethylethylene, thenylmethylethylene, pyridylmethylethylene, and indolylmethylethylene.

The "divalent aromatic hydrocarbon group" may be monocyclic or polycyclic, such as phenylene naphthylene, which is a lower alkyl group with 1 to 4 aromatic rings. May be replaced.

Furthermore, "divalent aromatic heterocyclic group" includes a heterocyclic group with aromatic unsaturation that contains at least one hetero atom selected from nitrogen, oxygen, and ionic atoms in the ring. The heterocyclic group may further form a fused ring with an aromatic hydrocarbon ring as described above.

Specific examples of such divalent aromatic heterocyclic groups are as follows.

Pyridinediyl, pyrimidinediyl, pyridazinediyl, pyridinediyl, furandiyl, thiophenediyl,
Quinolinediyl, isoquinolinediyl, benzofurandiyl, penzothiophenediyl, penzoxazolediyl, penzthiazolediyl, indolediyl, etc.

Among the compounds provided by the present invention, preferable ones include, in the general formula (1), Rl and R2 are the same or different and each is a hydrogen atom; a lower alkyl group, especially a t-butyl group; a halogen atom, Benzyl groups optionally substituted with lower alkoxy groups, nitro groups or cyano groups, in particular benzyl, p-methoxybenzyl, 0-nitrobenzyl, p-nitrobenzyl, p-chlorobenzyl, O-chlorobenzyl, p -cyanobenzyl group;
diphenylmethyl group; allyl group; cinnamyl group; tetrahydrobilanyl, tetrahydrothiopyranyl, 4
- a heterocyclic group selected from methoxytetrahydropyranyl, 4-methoxytetrahydrohithiopyranyl, tetrahydrofuranyl and tetrahydrothiofuranyl; or an acetyl group, especially acetyl, propionyl, phenylacetyl, chlorodiphenylacetyl, 3- Phenyl pionyl, 3-penzoyl pionyl, isobutyroyl, pivaloyl, 2-butenoyl, (E)-2-methyl-
2-butenoyl, benzoyl, 2-chlorobenzoyl,
3-nitrobenzoyl, 2-fluorobenzoyl, 3-trifluoromethylbenzoyl, 3-trichloromethylbenzoyl, 4-phenylbenzoyl, 2.4.6-}rimethylbenzoyl, α-naphthoyl, or R1 and R2 are taken together 1-t-butylethylidene,
1-phenylethylidene, isopropylidene, butylidene, cyclopentylidene, cyclohexylidene, cycloheptylidene, penzylidene, p-methoxybenzylidene, 2,4-dimethoxybenzylidene,
Represents a ylidene group selected from p-dimethylaminobenzylidene and 0-nitrobenzylidene, R3 is +1) C5~ having a linear or branched chain at the 1-position
CZS alkyl groups, especially pentyl, 1-isoprobylpentyl, 1-t-butylpentyl, hexyl, 1-isopropyhexyl, 1-t-butylhexyl, hebutyl, 1-isopropyheptyl, 1-t-butylheptyl, octyl , 1-t-butyloctyl, nonyl, 1-isobutylnonyl, decyl, 1-ethyldecyl, 1,1-
Jetyldecyl, 1-t-butyldecyl, undecyl,
1-isoprobylundecyl, 1,1-diethylundecyl, dodecyl, 1-t-butyldodecyl, 1-isoprobildodecyl, 1,1-jetyldodecyl, tridecyl, 1.1-diethyltridecyl, 1- t-p57 Tiltridecyl, tetradecyl, 1-isobutyltetradecyl, pentadecyl, 1-methylpentadecyl, II
1-dimethylpentadecyl, 1-ethylpentadecyl,
1.1-diethylpentadecyl, 1-isoprovirbentadecyl, 1-t-butylpentadecyl, hexadecyl, 1,1-dimethylhexadecyl, ■-methylhexadecyl, 1-ethylhexadecyl, 1-isopropyl Hexadecyl, 1-t-butylhexadecyl, heptadecyl, 1-methylheptadecyl, 1.1-dimethylheptadecyl, 1-ethylhebutadecyl, l-isopropylheptadecyl, 1-t-butylheptadecyl, octadecyl , 1-methyloctadecyl, 1.1-dimethyloctadecyl, 1-ethyloctadecyl or 1,1-diethyloctadecyl group; (2) CI2 to CIl+ alkenyl group that is linear or has a branched chain at the 1-position, especially 1
．． 1-dimethyl-9-decenyl, 1-ethyl-9-decenyl, 1-methyl-6-undecenyl, 1,1-dimethyl-6-undecenyl, 6-tridecenyl, 1-methyl-658 tridecenyl, 1,1-dimethyl- 6-tridecenyl, 8-tridecenyl, 1-methyl-8-tridecenyl,
1,1-dimethyl-8-tridecenyl, 10-tridecenyl, 1-methyl-10-tridecenyl, 1,1-
Dimethyl-10-tridecenyl, 10-pentadecenyl, 1-methyl-10-pentadecenyl, 1+1-dimethyl-10-pentadecenyl, 8-pentadecenyl, 1-
Methyl-8-pentadecenyl, 1+1-dimethyl-8-
Pentadecenyl, 12-hebutadecenyl, 1-methyl-
12-hebutadecenyl, 1,1-dimethyl-1, 2-hebutadecenyl, 10-hebutadecenyl, 1-methyl-1
0-hebutadecenyl, 1,1-dimethyl-10-hebutadecenyl, 8-hebutadecenyl, ■-methyl-8-hebutadecenyl, 1.1-dimethyl-8-hebutadecenyl,
1-ethyl-8-hebutadecenyl, 8.11-hebutadedyenyl, 1-methyl-8,11-hebutadecadienyl or 8,11.14-heptadecatrienyl group;
(31 C8-CIll-alkyl-04-C6 cycloalkyl group, especially 1-octylcyclobutyl, 15
9 Nonylcyclobutyl, 1-decylcyclobutyl, 1-undecylcyclobutyl, 1-dodecylcyclobutyl, 1
-pentadecylcyclobutyl, 1(9-octadecenyl)cyclobutyl, ■-octylcyclobentyl, ■1-decylcyclopentyl, 1-dodecylcyclopentyl, 1
-tridecylcyclopentyl, 1-tetradecylcyclobentyl, 1-(9-octadecenyl)cyclopentyl, 1-nonylcyclohexyl, 1-undecylcyclohexyl, 1-hexadecylcyclohexyl or 1-
(9-octadecenyl)cyclohexyl group; or (4) an amino group having a total of 8 to 20 carbon atoms mono- or di-substituted with an alkyl group or alkenyl group, such as 1-isopropylbentylamino, 1-t-butyl Pentylamino, 1-isopropylhexylamino, 1-t-
Butylhexylamino, 1-isopropylheptylamino, 1-t-butylheptylamino, 1-t-butyloctylamino, 1-isobutylnonylamino, decylamino, 160-ethyldecylamino, 1.1-diethyldecylamino, 1-t -butyldecylamino, undecylamino,
1-isopropyldodecylamino, 1,1-diethylundecylamino, dodecylamino, 1,-t-butyldodecylamino, 1-isopropyldodecylamino, 1
, 1-diethyldodecylamino, tridecylamino,
■,1-diethyltridecylamino, 1-t-butyltridecylamino, tetradecylamino, ■-isobutyltetradecylamino, pentadecylamino, 1-methylpentadecylamino, 1,1-dimethylbentadecylamino, 1 -ethylpentadecylamino, 1,1 -
Diethylpentadecylamino, ■-Isoprobylpentadecylamino, 1-t-butylpentadecylamino, hexadecylamino, 1,1-dimethylhexadecylamino, 1-methylhexadecylamino, 1-ethylhexadecylamino, ■ -Isoprobylhexadecylamino, 1-t-butylhexadecylamino, heptadecylamino, 1-methylheptadecylamino, 1,1-dimethylhebutadecylamino, 1-ethylheptadecylamino, 1-isopropyl Hebutadecylamino, 1-t-butylheptadecylamino, octadecylamino, 1methyloctadecylamino, 1.1-dimethyloctadecylamino, 1-ethyloctadecylamino, 1.1-diethyloctadecylamino, 1.1-dimethyl- 9-decenylamino, 1
-Ethyl-9-decenylamino, 1-methyl-6-undecenylamino, 1l1-dimethyl-6-undecenylamino, 1-methyl-6-tridecenylamino, 1.1
-dimethyl-6-tridecenylamino, 8-tridecenylamino, 1-methyl-8-tridecenylamino, 1
, 1-dimethyl-8-tridecenylamino, 10-tridecenylamino, ■-methyl-10-tridecenylamino, 1l1-dimethyl-10-tridecenylamino, 10-pentadecenylamino, 1 -Methyl-10-pentadecenylamino, 1l1 -dimethyl-10-pentadecenylamino, 8-pentadecenylamino, 1-methyl-8-pentadecenylamino, 1,1-dimethyl-
8-pentadecenylamino, 12-heptadecenylamino, 1-methyl-12-heptadecenylamino, 1,1-dimethyl-12-heptadecenylamino, 10-heptadecenylamino Cenylamino, 1-methyl-10-hebutadecenylamino, 1,1-dimethyl-IO-heptadecenylamino, 8-hebutadecenylamino, ■-Methyl-8-hebutadecenylamino ,1,1-
Dimethyl-8-hebutadecenylamino, 1-ethyl-8
-heptadecenylamino, 8.11-hebutadecadienylamino, ■Methyl-8,l1-hebutadecenylamino, 8. IL14-hebutadecatrienylamino, 1
-hexylcyclobutylamino, 1-heptylcyclobutylamino, ■-octylcyclobutylamino, 1-nonylcyclobutylamino, 1-decylcyclobutylamino, 1-undecylcyclobutylamino, 1-dodecylcyclobutylamino, 1-pentadecylcyclo butylamino, 1-(9-octadecenyl)cyclobutylamino,
■-pentylcyclopentylamino, 1-hexylcyclopentylamino, 1-heptylcyclopentylamino, 163 octylcyclopentylamino, 1-decylcyclopentylamino, ■-dodecylcyclopentylamino, 1-
Tridecylcyclopentylamino, 1-tetradecylcyclobentylamino, 1(9-octadecenyl)cyclobentylamino, 1-nonylcyclohexylamino, ■
-undecylcyclohexylamino, ■-hexadecylcyclohexylamino, 1-(9-octadecenyl)cyclohexylamino, decylhexylamino, octylpropylamino, hexyloctylamine, (1-butyloctyl)hexylamino, hexyldecylamino ,
(1-ethyldecyl)butylamino, (Ll-diethyldecyl)pentylamino, butylundecylamino, butyldodecylamino, probyltetradecylamino, butylpentadecylamino, (1-methylpentadecyl)
butylamino, (1,1-dimethylpentadecyl)propylamino, ethylhexadecylamino, ethyl (1-
Methylhexadecyl)amino, (1.1dimethylhexadecyl)methylamino, hepta64 decylmethylamino, (1-methylheptadecyl)methylamino, (l,■-dimethylhebutadecyl)methylamino, methyloctadecylamino, Ethyl (1-methyloctadecyl)amino, ethyl (1,1-dimethyloctadecyl)amino, (1.1dimethyl-9-decenyl)
Butylamino, (1ethyl-9-decenyl)propylamino, bentyl(6-undecenyl)amino, (1-methyl-6-undecenyl)butylamino, (1l1-dimethyl-6-undecenyl)propylamino, pentyl(6-tridecenyl) )amino, (l-methyl-6-tridecenyl)pentylamino, (Lldimethyl-6-tridecenyl)ethylamino, butyl (8-tridecenyl)
Amino, butyl (1 methyl-8-tridecenyl) amino, (1,1 dimethyl-8-tridecenyl) ethylamino, ethyl (10-tridecenyl) amino, butyl (1 methyl-10-tridecenyl) amino, (1,l- dimethyl-10-tridecenyl)propylamino, butyl (1
0-pentadecenyl)amino, butyl(165 methyl-10-pentadecenyl)amino, (Ll-dimethyl-10-pentadecenyl)propylamino, (8-
pentadecenyl)propylamino, (1-methyl-8-
pentadecenyl)propylamino, ethyl(1,1-dimethyl-8-pentadecenyl)amino, butyl(12-
hebutadecenyl)amino, ethyl(1-methyl-12-
hebutadecenyl)amino, (1,1-dimethyl-12-
heptadecenyl)propylamino, ethyl(10-hebutadecenyl)amino, (1-methyl-10-hebutadecenyl)propylamino, ethyl(1,1-dimethyl-1
0-hebutadecenyl)amino, (8-hebutadecenyl)
Methylamino, methyl(1-methyl-8-hebutadecenyl)amino, ethyl(1.1-dimethyl-8-hebutadecenyl)amino, (1-ethyl-8-hebutadecenyl)
Pro and Ruamino, (8. 11-hebutadecadienyl)
66 A represents (11 linear or branched 02 to CI 'O alkylene groups, such as ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene, heptamethylene, octamethylene, nonamethylene, decamethylene,
propylene, ethyl ethylene, isopropylene,
Propyl ethylene, butyl ethylene, isobutyl ethylene, 1-methyltrimethylene, ■-ethyltrimethylene, 1-isopropyltrimethylene, 1-isobutyltrimethylene, 1-methyltetramethylene L/n, l-isopropyltetra Methylene or l-isobutyltetramethylene; (21 CS~C, cycloalkyl-02~C, alkylene group, such as cyclobentylethylene, cyclohexylethylene, cycloheptylethylene, 1-cyclopentyltrimethylene, ■cyclohexyltrimethylene, 1 -cyclopentyltetramethylene or 1-cyclohexyltetramethylene; 67 (31 CS-C7 cycloalkylene group, e.g. 1
, 2-cyclobentylene, 1,3-cyclopentylene,
1,2-cyclohexylene, 1,3-cyclohexylene, 1,4-cyclohexylene, I+2 cycloheptylene, 1,3-cycloheptylene or 1,4-cycloheptylene; (41 C4-C8 alkenylene or C, ~ C8
Alkynylene groups, e.g. 2-butenylene, 1-methyl-
2-butenylene, 1-ethyl-2-butenylene, 1-propylbutenylene, 1-butylbutenylene, 2-butynylene, 2-pentenylene, 2-pentynylene, 2-hexenylene, 3-hexenylene, 2-hexynylene, 3-
Hexynylene, 2-hebutenylene, 3-heptenylene,
2-heptynylene, 3-heptynylene, 2-octenylene or 4-octenylene; (5) Cs-C, cycloalkylene 7 CI''Cs alkylene group, e.g. 1
,1-pentamethyleneethylene, 1l1-tetramethyleneethylene, ■,l-hexamethyleneethylene, Ll
-dimethyl68 ethylene, 1,l-tetramethylene trimethylene, 1.
1-pentamethylene trimethylene, 1.2-}rimethylene trimethylene or 1,2-tetramethylene trimethylene; (6) 02-C5 alkylene group substituted with an aryl or heteroaryl group, such as phenylethylene,
naphthylethylene, furylethyne, chenylethylene,
pyridylethylene, benzylethylene, naphthylmethylethylene, furylmethylethylene, thenylmethylethylene, pyridylmethylethylene, indolylmethylethylene; or (7) represents O-phenylene, m-phenylene or p-phenylene; CI. A compound in which either one of X and Y represents 1NH1 or 1N-, and the other represents -0-, -S-, -NH1 or CH31N-, and 69 n is an integer of 1 to 4 can be mentioned.

Thus, representative examples of the compound represented by the general formula (I) provided by the present invention are as follows.

N-(4-(oleoyloxy)phenyl]-3(
N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carponyl)amino]propanamide N
- C4- (oleoyloxy)phenyl]-3(N
-(2,4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanamide 4-(oleoylamino)phenyl 3-(N-(2, 2, 5.5
-tetramethyl-1,3-dioxane-4carbonyl)
Amino]propionate 4-(oleoylamino)phenyl 3-(N-(2.
4-dihydro 3,3-dimethyl-1-oxobutyl)
Amino]propionate N- (4- (oleoylthio)phenyl)-3-(
N-(2, 2, 5. 5-tetramethyl-1.3
-dioxane-4-carbonyl)amino]propanamide 70 N-(4-(oleoylthio)phenyl)-3(N-
(2.4-dihydroxy-3.3-dimethyl-1oxobutyl)amino]propanamide S-4(oleoylamino)phenyl 3-(N-(2, 2, 5. 5-tetramethyl-1.3- dioxane-4carbonyl)amino]propanethioate S-4- (oleoylamino)phenyl 3(N-(2,4-dihydro-3,3-
Dimethyl-1-oxobutyl)amino]propanethioate N- (2- (oleoylamino)phenyl)-
3(N-(2,2,5.5-tetramethyl-1.3
-dioxane-4-carponyl)amino]propanamide 2-(oleoylamino)phenyl 3-[N(2,
2,5.5-tetramethyl-1,3-dioxane-4carbonyl)amino]propionate N-(2-(oleoyloxy)phenyl]-3(N
- (2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanamide N-
(2-(linoleoylamino)phenyl]3-
(N-(2,2,5.5-tetramethyl-1,3-dio71xane-4-carbonyl)amino]propanamide+1-(2-(linolenoylamino)phenyl)3
- (N-(2,2.5.5-tetramethyl-1.3-
Dioxane-4-carbonyl)amino]propanamide N-(2-(stearoylamino)phenyl)3-
(N-(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide N- C2- (lauroylamino)phenyl]-3-
(N-(2.2,5.5-tetramethyl-1.3
-dioxane-4-carbonyl)amino]propanamide N- (2- (octanoylamino)phenyl]3
- (N - (2,2,5.5-tetramethyl-1
．． 3-dioxane-4-carbonyl)amino]propanamide N- (3- (linoyl amino) phenyl]-3-
(N-(2.2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide 7
2 N- (4- (lauroylamino)phenyl]-3-
(N-(2,2.5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanamide 4
-(linoylamino)phenyl)3-(N(2,2,
5.5-tetramethyl-1,3-dioxane 4-carbonyl)amino]propionate N- [1- (oleoylamino)phenyl]-3- (N-(2,4-diacetoxy3.3-dimethyl 1- oxobutyl)amino]propanamide N- (2- (oleoylamino)
Phenyl]-3- (N-(2,4-dihydroxy-3
．． 3-dimethyl-1-oxobutyl)amino]propanamide N-(3-(oleoylamino)phenyl)
-3(N-(2,4-diacetoxy3,3-dimethyl l-oxobutyl)amino]propanamide N-
(3-(oleoylamino)phenyl]-3(N-(
2.4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanamide N-(4-(oleoylamino)phenyl]-3(N-(2.4-diacetoxy-3.3-dimethyl)73 ■ -oxobutyl)amino]propanamide N- (4
-(oleoylamino)phenyl]-3[N-(2.
4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanamide 4-(oleoylamino)phenyl 3-[N(2,4-diacetoxy-3+3-dimethyl-1-oxobutyl)amino]probionate N- (4-(oleoyloxy)phenyl]-3(N
-(2,4-diacetoxy-3,3-dimethyl-1-oxobutyl)amino]propanamide S- (4- (oleoylamino)phenyl 3(N - (2,4-diacetoxy-3,3-dimethyl-1 -oxobutyl)amino]propanethioate N- (4-(oleoylthio)phenyl]-3[N-(2,4-diacetoxy3.3-dimethyl-1-oxobutyl)amino]propanamide 4-(oleoylamino) Phenyl 3-[N
(2,4-dibenzyloxy-3,3-dimethyl-1oxobutyl)amino]probionate N- (2-N-
oleoylaminoethyl)-374 (N-(2,4-diacetoxy3,3-dimethyl-1oxobutyl)amino]propanamide N-(3
-N-oleoylaminopropyl)-3(N-(2
,2,5.5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propanamide N-(1-N-
oleoylaminoethyl)-3-CN-(2,4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanamide 2-(N-oleoylamino)ethyl 3-[N(2,2,5 .5-tetramethyl-1,3
-dioxane 4-carbonyl)amine]propionate 2-(N-oleoylamine)ethyl 3-[N-(2
．． 4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]probionate 3-(N-oleoylamino)propyl 3-(N-
(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3-(N
-oleoylamino)propyl 3-(N-(2.4-
dihydroxy-3,3-dimethyl-1-oxobutyl)
Amino]propionate 75 3- (N-oleoylamino)propyl 3(N -
(2,4-diacetoxy3,3-dimethyl-1oxobutyl)amino]propionate 4-(N-oleoylamino)butyl 3-[N(2,2.5.5-tetramethyl-1,3-dioxane 4 -carbonyl)amino]
4-(N-oleoylamino)butyl propionate
3-(N(2l4-dihydroxy-3,3-dimethyl-
1-oxobutyl)amino]probionate S-2-(N-oleoylamine)ethyl 3(N-
(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanethionate S-2-(N-oleoylamino)ethyl 3-(N-
(2,4-dihydroxy-3,3-dimethyl-1oxobutyl)amino]propanethionate N-(3-oleoylaminopropyl)-3(N - (2,2,5.5
-tetramethyl-1,3-dioxane-4-carponyl)amino]propanamide N- (3-oleoylaminopropyl)-376 (N-(2,4-dihydroxy-3,3-dimethyl-l)
oxobutyl)amino]propanamide N-(3-
oleoylaminopropyl)-3(N-(2.4-
diacetoxy-3,3-dimethyl-1oxobutyl)amino]propanamide N-(4-oleoylaminobutyl)-1(N(2.2,5.5-tetramethyl-
1.3-dioxane-4-carbonyl)amino]propanamide N-(4-oleoylaminobutyl 13-(N
-(2,4-dihydroxy-3.3-dimethyl-1-oxobutyl)amino]propanamide N-(4-oleoylaminobutyl)-3-(N-(2
．． 4-Diacetoxy3,3-dimethyl-1-oxobutyl)amino)propanamide N-(6-oleoylaminohexyl)-3-(N-(
2.2.5.5-tetramethyl-1,3-dioxane-
4-carbonyl)amino]propanamide N-(5-oleoylaminopentyl)-3(N-(2.2,5.
5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanamide 77 N-(8-oleoylaminooctyl)-3(N-
(2,2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide N-(2
-oleoyloxyethyl)-3-(N(2,2,5.
5-tetramethyl-1.3-dioxane 4-carbonyl)amino]propanamide 5-(N-oleoylamino)pentyl) 3-(N-(2,2.5.5-tetramethyl-1.3- dioxane-4-carponyl)amino]propionate 6-(N-oleoylamino)hexyl) 3(N-(2, 2, 5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2 -(N-methyl-N-oleoylamino)ethyl 3- (N-(2,2,5.5-tetramethyl-I+3-dioxane-4-carbonyl)amino]propionate 3- (N-oleoylamino)propyl ) 3(N
-(2,4-dibenzyloxy-3,3-dimethyl1-
oxobutyl)amino]propionate 1(N-oleoylamino)propyl) 378 CN-C4-henzyloxy-2-hydroxy 3,3-
Dimethyl-1-oxobutyl)amino]brobionate 3-(N-oleoylamino)probyl 3(N- (
2-Hydroxy-3,3-dimethyl-4(trimethylacetyl)oxy-1-oxobutyl)amino]propionate 3-(N-oleoylamino)propyl 3(N-(2
-phenyl-5,5-dimethyl-1,3 dioxane-4
-carbonyl)amino]propionate 3-(N-oleoylamino)probyl 3(N- (
3,3-dimethyl-1,5-dioxaspiro(5,5
) - 3-carbonyl)amino]propioneto 3-(N-hexadecanoylamino)probyl 3-(N
-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3-(N-linoleoylamino)propyl 3-79 (N-(2,2,5.5 -Tetramethyl-1,3-dioxane-4-carponyl)amino]propionate 3-
(N-linolenylamino)propyl 3(N-(2,2
．． 5.5-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3-(N-octadecanoylamino)propyl 3-[N-(2,2,5.5
-tetramethyl-1,3-dioxane-4-carponyl)amino]propionate 3-(N-tetradecanoylamino)propyl 3-[
N-(2.2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propionate 3-(N-dodecanoyl)aminopropyl 3(N-
(2.2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3-N-
(decanoylamino)propyl 3[N - (2.2
．． 5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3-(N-octanoyl)aminoprovil 380 [N - (2,2,5.5-tetramethyl-1.3-
dioxane-4-carbonyl)amino]probionate 3-(N-hexanoylamino)propyl 3(N-
(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3- (
N-(2-isobrobylhexanoyl)amino]propyl 3-[N-(2.2,5.5-tetramethyl-
1.3-dioxane-4-carponyl)amino]propionate 3- (N- (2-t-butylhexanoyl)amino]propyl l- [N-(2,2,5.5-tetramethyl-1.3 -dioxane-4-carbonyl)amino]
Propionate 3- (N- (2-t-butylheptanoyl)amino]propyl 3- (N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carponyl)amino)
Propionate 3- (N- (2-t-butylnonanoyl)amino)
Propyl 3-(N-(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]p81 Ropionate 3-(N-(2,2-diethylundecanoyl)amino) Propyl 3-CN-(2,2,5.5
-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3= (N- (2-isoprobildeccanoyl)amino]propyl 3 - (N-(2,2,5.5-tetramethyl- 1,3-dioxane-4-carbonyl)amino]propionate 3-[N-(2-t-butyltetradecanoyl)amino]propyl 3-(N-(2.2,5.5-tetramethyl-1. 3-dioxane-4-carbonyl)amino]propionate 3-(N-(2-t-butylhexadecanoyl)amino]propyl 3-(N-(2.2.5.5-
tetramethyl-1,3-dioxane-4-carbonyl)
Amino]propionate 3- (N- (2-isoprobylheptadecanoyl)
Amino]propyl 3- (N-(2.2.5.5-tetramethyl-1,3-dioxane-4-carbonyl)a82 Mino]propionate 3- (N- (2-ethyloctadecanoyl)amino) Propyl 3-(N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carponyl)amino]
Propionate 3-(N-(2,2-dimethyl-10-undecenoyl)amino]propyl 3-(N-(2,2,
5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3-(N-(2,2-dimethyl-7-dodecenoyl)amino]propyl 3-(N-(2.2.5 .5
-tetramethyl-1,3-dioxane-4-carponyl)amino]propionate 3 - (N- (2,2-dimethyl-7-tetradecenoyl)amino]propyl 3 - (N - (2
,2,5,5tetramethyl-1,3-dioxane-4-
carbonyl)amino]propionate 3-(N-(2,2-dimethyl-9-tetradecenoyl)amino]propyl 3-(N-(2,2,
5,5 Tetramethyl-1,3-dioxane-4-carboni83 Probionate 2,2-dimethyl-11-tetradecenopropyl 3-
CN-<2.2.5.51,3-dioxane-4-carponipropionate 2,2-dimethyl-11-pentadecenopropyl 3
- (N-(2,2,5,51,3-dioxane-4-
Carbonipropionate 2,2-dimethyl-9-pentadecenopropyl 3-(If-(2,2,5,51,3-dioxane-4-carbonipropionate 2,2-dimethyl-9- xadecenopropyl 3-(N-(2,2,5,51,3-dioxane-4-carbonipropionate 2.2-dimethyl-9-hebutadecenopropyl 3-(N-(2, 2.5,51,3-dioxane-4-carbonyl)amino] 3- (N- (yl)amino] tetramethyll)amino] 3- (N- (yl)amino] tetramethyll)amino] 3-.[N- (yl)amino]tetramethyll)amino]3-CN-(yl)amino]tetramethyll)amino]3-(N-(yl)amino)tetramethyl84l)amino]propionate 3-(N-(2.2- Dimethyl-9-octadecenoyl)amino]propyl 3-(N-(2,2
, 5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 3- (N- (2-methyl-9-octadecenoyl)
Amino]propyl 3-CN-(2,2,5.5-tetramethyl-13-dioxane-4-carbonyl)amino]propionate N- (2-(oleoylamino)cyclohexane-
1-yl)-3- (N { (2R)-2,4-diacetoxy-3,3-dimethyl-1-oxobutyl}amino]propanamide N- [(Is.23)-2- (oleoylamino)
cyclohexan-1-yl)-3- [N-{ (2R
)-2,4-diacetoxy-3,3-dimethyl-1oxobutyl}amino]propanamide N- ((IR,
2R)-2-(oleoylamino)cyclohexane-
1-yl) -3- (N- { (2R)-2.4-
dihydroxy-3,3-dimethyl-185 monooxobutyl}amino]propanamide N-((Is
,2S)-2- (oleoylamino)cyclohexan-1-yl) -3- (N- ( (2R) -2.
4-dihydroxy-3,3-dimethyl-1-oxobutyl}amino]propanamide N- (2- (oleoylamino)cyclohexan-1-yl)-3- (N-(
2.4-Diacetoxy3,3-dimethyl-1-oxobutyl)amino]bropanamide N-(2-(oleoylamino)cyclohexane-1
-yl) -3- (N (2.4-diacetoxy=3
,3-dimethyl-1-oxobutyl)amino]propanamide N- ((Is,23)-2- (oleoylamino)
cyclohexan-1-yl) - 3 - (N -
3-(N -(2,2,5,5tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate (Is 2S)-2- (oleoylamino)cyclohexan-1-yl 3 (N-(2 ,2.5.5
-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate (IR,2R)-2- (stearoylamino)cyclohexan-1-yl 3-[N-(2,2,5,5tetramethyl- 1.3-Dioxane-4-carbonyl)amino]propionate (Is.2S)-2- (linoleoylamino)cyclohexan-1-yl 3- (N-(2,2.5,5tetramethyl-1. 3-Dioxane-4-carbonyl)amino]propionate 2-(1-octylcyclobutanoylamino)cyclohexan-1-yl 3-(N-(2.2,5.5-tetramethyl-1,3-dioxane- 4-carbonyl)amino]propionate 2-(1-nonylcyclobutanoylamino)cyclohexan-1-yl 3-(N-(2.2,5.5-
tetramethyl-1,3-dioxane-4-carbonyl)
87 Amino]probionate 2-(oleoylamino)cyclopencun-1-yl
i (N-(2,2,5.5-tetramethyl-1.3-
dioxane-4-carbonyl)amino]probionate 2-(oleoylamino)cyclohebutan-1yl 3
- (N-(2,2,5.5-tetramethyl-1.3dioxane-4-carbonyl)amino]probionate 3-(oleoylamino)cyclohexane-lyl 3
- (N-(2,2,5.5-tetramethyl-1,3dioxane-4-carponyl)amino]probionate 4-(oleoylamino)cyclohexane-1-yl
3-[N-(2,2,5.5-tetramethyl-1.3
dioxane-4-carbonyl)amino]propionate 2-(1-decylcyclobutanoylamino)cyclohexan-1-yl 3- (N-(2,2,5.5-tetramethyl-1,3-dioxane-4- carbonyl)88 amino]propionate 2-(1-undecylcyclobutanoylamino)cyclohexan-1-yl 3-(N-(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino ]Propionate 2-(1-pentadecylcyclobutanoylamino)cyclohexan-1-yl 3-(N-(2,2,5.5
1-tetramethyl-1,3-dioxane-4-carponyl)amino]propionate 2-(1-(9-octadecenyl)cyclobutanoylamino)cyclohexan-l-yl 3(N-(
2.2.5.5-Tetramethyl-1,3-dioxane-
4-carbonyl)amino]probionate 2-(1-decylcyclobentanoylamino)cyclohexane-1-
yl 3-(N-(2,2,5,5tetramethyl-1
．． 3-Dioxane-4-carponyl)amino]probionate 2-(1-}lidecylcyclopentanoylamino)cyclohexan-1-yl 3-(N-(2,2,5,5
Tetramethyl-1,3-dioxane-4-carboxylic)amino]propionate 2-(1-decylcyclohexanoylamino)cyclohexan-1-yl 3-(N-(2,2,5,
5tetramethyl-1.3-dioxane-4-carbonyl)amino]propionate 2-(1-nonylcyclohexanoylamino)cyclohexan-1-yl 3-[N-(2.2,5.
5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1-(9-octadecenyl)cyclohexanoylamino)cyclohexan-1-yl 3-(N-
(2.2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1
-isoprobylpentylcarbamoylamino)cyclohexan-1-yl 3-(Nl2.2,5.5-tetramethyl-1,3-dioxane-4carbonyl)amino]
Probionate 2-(1-isoprobylhexylcarbamoylamino)
Cyclohexan-1-yl 3-(N-(2.2.5.
5-tetramethyl-1,3-dioxane-490 carponyl)amino]propionate 2- (1-t-butyldodecylcarbamoylamino)
Cyclohexan-1-yl i CN-C2.2.5,
5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(Ll-dimethylhexadecylcarbamoylamino)cyclohexan-1-yl 3-[N(2,2.5.
5-tetramethyl-1,3-dioxane-4carponyl)amino]propionate 2-(octadecylrubamoylamino)cyclohexan-1-yl 3-(N-(2,2.5 5-tetramethyl-1,3-dioxane) -4-carbonyl)amino]propionate 2-(Ll-dimethyloctadecylcarbamoylamino)cyclohexan-1-yl 3-(N(2,2,5.
5-tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1,1-dimethyl-9-decenylcarbamoylamino)cyclohexan-1-yl 3-[N(2,2,
5.5-Tetramethyl-1,3-dioxane 91 4-carbonyl)amino]propionate 1(1.1-
Dimethyl-6-undecenylcarbamoylamino)cyclohexan-1-yl 3(N - (2.2,5.5
-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 1-(Ll-dimethyl-8-
tridecenylcarbamoylamino)cyclohexane-1
-yl 3(N-(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]probionate 2-(1-methyl-10-bentadecenylcarbamoylamino)cyclohexane-1 -il 3CN
- (2,2,5.5-tetramethyl-13-dioxane-4-carbonyl)amino]probionate 2-(
1,1-dimethyl-10-hebutadecenylcarbamoylamino)cyclohexan-1-yl 3CN - (2
,2.5.5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]probionate 2-(1-methyl-8-pentadecenylcarbamoylamino)cyclohexan-1-yl 3(N-(2,2,5.5-tetramethyl-1,3-dioxa92) 4-carbonyl)amino]propionate 2-(8
-octadecenylcarbamoylamino)cyclohexan-1-yl 3-(Ni2,2 5,5tetramethyl-1,3-dioxane-4-carponyl)amino]probionate 2-(8.11-octadecadienylcarbamoylamino) Cyclohexan-1-yl 3-(N-(2,2,
5.5-tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1-methyl-8,IL14-octadecatrienylcarbamoylamino)cyclohexan-1yl 3
-CN-(2,2,5.5-tetramethyl-1,
3dioxane-4-carbonyl)amino]propionate 2-(1-hexylcyclobutylcarbamoylamino)
Cyclohexan-1-yl. 3-(N-(2,2,5
．． 5-Tetramethyl-1,3-dioxane-4carbonyl)amino]probionate 2-(1-octylcyclobutylcarbamoylamino)
Cyclohexan-1-yl 3-(N-(2,93 2,5.5-tetramethyl-1,3-dioxane-4carbonyl)amino)probionate 2-(1-octylcyclopentylcarbamoylamino)cyclohexane-1 -yl 3-[N(2,2,5.
5-tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1-octylcyclohexylcarbamoylamino)cyclohexan-1-yl 3-[N(2,2,5.
5-Tetramethyl-1,3-dioxane-4carponyl)amino]propionate 2-(1-heptylbenthylcarbamoylamino)cyclohexan-1-yl 3-(N(2.2.5.
5-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1-decylcyclopentylcarbamoylamino)cyclohexan-1-yl 3-(N-(2,2.5.5-tetramethyl -1.3
-dioxane-4carbonyl)amino]propionate 2-(1-hexylcyclohexylcarbamoylamino)cyclohexan-1-yl 3-(N-94 (2,2.5.5-tetramethyl-1,3-dioxane- 4-carponyl)amino]propionate 2- (1- (6-hexadecenyl)cyclohexylcarbamoylamino]cyclohexan-1-yl 3-
(N-(2,2,5.5-tetramethyl-1,3dioxane-4-carbonyl)amino]propionate 2- (1-(6-hexadecenyl)cyclobutylcarbamoylamino)cyclohexan-1-yl 3- (
N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1-(6-hexadecenyl)cyclopentylcarbamoylamino)cyclohexan-1-yl 3
- (N - (2,2,5.5-tetramethyl-1,
3-dioxane-4-carbonyl)amino]propionate 2-(decylhexylcarbamoylamino)cyclohexan-1-yl 3-(N-(2,2,5.5
-tetramethyl-1,3-dioxane-4-carponyl)95 amino]probionate 2-(hexyloctylcarbamoylamino)cyclohexan-1-yl 3-(N-(2,2,5,5
tetramethyl-1,3-dioxane-4-carbonyl)
Amino]probionate 2-(butyldodecylcarbamoylamino)cyclohexan-1-yl 3-(N-(2.2.5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino)propionate 2-( methyloctadecylcarbamoylamino)cyclohexan-1-yl i (N-(2,2,5,5tetramethyl-1,3-dioxane-4-carponyl)amino]propionate 2-[butyl(1,1-dimethyl-6 -undecenyl)
Carbamoylamino]cyclohexane-1yl 3 -
[N-(2,2,5.5-tetramethyl-1,3dioxane-4-carbonyl)amino]probionate 2-[butyl(1,1-dimethyl-8-tridecenyl)
carbamoylamino]cyclohexane-196yl 3-(N-(2,2,5.5-tetramethyl-
1.3-dioxane-4-carbonyl)amino]propionate 2-(butyl(1-methyl-10-pentadecenyl)carbamoylamino)cyclohexan-1-yl 3-
(N-(2,2,5.5-tetramethyl-1.3-
dioxane-4-carbonyl)amino]probionate 2-(.(8-pentadecenyl)propylcarbamoylamino)cyclohexan-1-yl 3(N - (2
．． 2.5.5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propionate 2-[butyl(
1.1-dimethyl-8-hebutadecenyl)carbamoylamino]cyclohexan-1yl i (Nl2,2.
5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-[ethyl(1,1-dimethyl-8-heptadecenyl)carbamoylamino]cyclohexane-1-yl 3
- (N-(2.2.5.5-tetramethyl-1,9
7 3-dioxane-4-carbonyl)amino]probionate 2-methyl-2-(N-oleoylamine)ethyl 3
- (N-(2.2.5.5-tetramethyl-1.3dioxane-4-carbonyl)amino]propionate 2-ethyl-2-(N-oleoylamino)ethyl 3
- (N-(2,2,5.5-tetramethyl-1.3-
dioxane-4-carponyl)amino]propionate 2-isopropyl-2- (N-oleoylamino)ethyl 3- (N-(2.2,5.5-tetramethyl-
1.3-Dioxane-4-carbonyl)amino]propionate 2-isobutyl-2-(N-oleoylamino)ethyl 3-(N-(2,2,5.5-tetramethyl-1.
3-Dioxane-4-carbonyl)amino]propionate 2,2-pentamethylene-2-(N-oleoylamino)ethyl 3-(N-(2,2,5.5-tetramethy98-1,3-dioxane) -4-carbonyl)amino]propionate 2-phenyl-2-(N-oleoylamino)ethyl
3-(N-(2,2,5.5-tetramethyl-
1.3Dioxane-4-carbonyl)amino]propionate 2-benzyl-2-(N-oleoylamino)ethyl
3-(N-(2,2,5.5-tetramethyl-1.
3dioxane-4-carbonyl)amino]propionate 2-naphthyl-2-(N-oleoylamino)ethyl
3-(N-(2,2.5.5-tetramethyl-1,
3-dioxane-4-carbonyl)amino]probionate 2-(2-furyl)-2-(N-oleoylamino)ethyl 3-(N-(2,2,5.5-tetramethyl1)
,3-dioxane-4-carponyl)amino]propionate 2-cyclopentyl-2-(N-oleoylamino)ethyl 3-CN-(2,2,5.5-tetramethyl99 1,3-dioxane-4- carbonyl)amino]propionate 2-(3-indolyl)methyl-2-(N-oleoylamino)ethyl 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carponyl) )amino]probionate 4-(N-oleoylamino)-2-butenyl 3-C
N-(2.2.5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 4-(N-oleoylamino)-2-butynyl 3-[
N-(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amine]propionate 2-(N-(1-undecylcyclobutanecarbonyl)amino)cyclobencun-1-yl 3( N-(2
,2.5.5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propionate 2- (N-
(1-pentadecylbutanecarbonyl)amino]
Cyclohebutan-1-yl 3100 CN - (2,2,5.5-tetramethyl-1,3-
dioxane-4-carponyl)amino]propionate i (N-(1-(9-octadecenyl)cyclobutanyl)amino]cyclohebutan-1yl 3
- (N-(2,2.5.5-tetramethyl-1,3-
Dioxane-4-carponyl)amino]propionate 2- (N-(1-decylcyclopenkunecarbonyl)
Amino]cyclopencun-1-yl 31(N - (
2.2,5.5-tetramethyl-1,3-dioxane-
4-carbonyl)amino]probionate 2-CN-
(1-}lidecylpentanecarbonyl)amino]
Cyclopentan-1-yl 3-CN~(2,2.5
．． 5-Tetramethyl-L3-dioxane-4-carbonyl)amine]propionate 2-(N-(1-decylcyclohexanecarbonyl)amino)cyclobentane-
1-yl 3-(N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(N-(1-nonylcyclohexanecarbonyl) Amino]cyclohebutan-1-yl 3(N -
(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2- (N
- (1-(9-octadedenyl)cyclohexanecarponyl]amino]cyclopentan-1-yl l- (
N-(2.2.5.5-tetramethyl1,3-dioxane-4-carbonyl)amino]probionate 2-(N-(1-isoprobylpentylcarbamoyl)amino]cyclohebutan-1-yl 3-( N-
(2.2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1
-isoprobylhexylcarbamoylamino)cyclohebutan-1-yl i(N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2- (1-t- butyldodecylcarbamoylamino)
Cyclopencun-1-yl 3- (N-(2,2,5
,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 102 2-(Ll-dimethylhexadecylcarbamoylamino)cyclohebutan-1-yl i(N(2,2,5.5
-tetramethyl-1,3-dioxane-4-carponyl)amino]propionate 2-(octadecylcarbamoylamino)cyclopencun-1-yl 3-(N
-(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propionate 1-(LL-dimethyloctadecylrubamoylamino)cyclohebutan-1-yl 3-[N(2. 2.5.
5-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1,1-dimethyl-
9-decenylcarbamoylamino)cyclohebutane-1
-yl 3-(N(2,2,5.5-tetramethyl-1
,3-dioxane 4-carbonyl)amino]propionate 2-(1,1-dimethyl-6-undecenylcarbamoylamino)cyclohebutan-1-yl 3CN -
(2.2.5.5-tetramethyl-1.3-dioxane-4-carponyl)amino]propionate 2-(L
l-dimethyl-8-tridecenylcarbamoylamino)
Cyclohebutan-1-yl 3(N - (2.2,5
．． 5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(1-methyl-10
-pentadecenylcarbamoylamino)cyclopentan-l-yl 3-(N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 1-(Ll-dimethyl-10- heptadecenylcarbamoylamino)cyclopencun-1-yl
3CN-(2,2,5.5-tetramethyl-1.3-
dioxane-4-carbonyl)amino]propionate 2-(1-methyl-8-hebutadecenyl-bentan-1-yl l-(N-(2,2,5
．． 5-tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(8-octadecenylcarbamoylamino)cyclopencun-1-yl 3-(N-(2.2,5,5tetramethyl-1 ,3-dioxane-4-carbonyl)amino]propionate 2-(811-octadeylcarbamoylamino)cyclopencun-1-yl 3-(N-(2.2,5
．． 5-Tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1-methyl-8,IL14-octadecatrienylrubamoylamino)cyclopencun-1yl 3
- CN-(2.2.5.5-tetramethyl-1,3dioxane-4-carbonyl)amino]propionate 2-(1-hexylcyclobutylcarbamoylamino)
cyclohebutan-1-yl 3-(N-(2,2.5.
5-Tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1-octylcyclobutylcarbamoylamino)
Cyclohebutan-1-yl 3-(N-(22, 5.
5-tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1-octylcyclopentylcarbamoylamino)cyclohebutan-1-yl 3-[N(2,2,5.
5-tetramethyl-1,3-dioxane-41 0 5 monocarbonyl)amino]propionate 2-(1-octylcyclohexylcarbamoylamino)cyclohebutan-1-yl 3-[N-(2.2.5.5-tetramethyl -1,3-dioxane-4carbonyl)amino]propionate 2-(l-heptylcyclopentylcarbamoylamino)cyclopentan-1-yl 3-(N-(2,2.5
．． 5-Tetramethyl-1,3-dioxane-4carbonyl)amino)propionate 2-(1-decylcyclopentylcarbamoylamine)
Cyclopentan-1-yl 3-(N-(2.2,5.
5-Tetramethyl-1,3-dioxane-4carbonyl)amino]propionate 2-(1-hexylcyclohexylcarbamoylamino)cyclohebutan-1-yl 3-[N(2, 2,
5. 5-tetramethyl-1,3-dioxane-4carbonyl)amino]probionate 2- (1- (6-hexadecenyl)cyclohexylcarbamoylamino)cyclopentan-1-yl 3-
(N-(2.2.5.5-tetramethyl-1.31 0
6 dioxane-4-carbonyl)amino]propionate 2- (1- (6-hexadecenyl)cycloptylcarbamoylamino)cyclohebutan-1-yl 3-
(N-(2,2,5.5-tetramethyl-1,3-
dioxane-4-carponyl)amino]probionate 2-(1-(6-hexadecenyl)cyclopentylcarbamoylamino)cyclohebutan-1-yl 3
- (N-(2.2.5.5-tetramethyl-1.3dioxane-4-carbonyl)amino]probionate 2-(decylhexylcarbamoylamino)cyclopentan-1-yl 3 - [N - (2 .2.5.5
-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(hexyloctylcarbamoylamino)cyclohebutan-1-yl 3-(N-(2,2,5.5-
tetramethyl-1,3-dioxane-4-carbonyl)
Amino]propionate 2-[butyl(1,1-dimethyl-8-hebutadecenyl)carbamoylamino)cyclobencun-1yl 3
- (N - (2,2,5.5-tetramethyl-1,
3-Dioxane-4-carbonyl)amino]propionate 2-methyl-2-(N-linoleoylamino)ethyl
3-CN-(2,2,5.5-tetramethyl-
1.3 dioxane-4-carbonyl)amino]probionate 2-methyl-2- (N- (2-isoprobylhexanoyl)amino]ethyl 3- (N-(2,2.5,
5 Tetramethyl-1,3-dioxane-4-carbonyl)amino)propionate 2-methyl-2-,(N-(2-t-butylheptanoyl)amino]ethyl 3-(N-(2,2,5 ,5
tetramethyl-1,3-dioxane-4-carbonyl)
Amino]propionate 2-methyl-2-CN- (2.2-jethylundecanoyl)amino]ethyl 3- (N-(2.2.
5,5tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-methyl-2-[N-(2.2-1-rimethylenedecanoyl)amino]ethyl l-(N-(2
,2,5,5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propionate 2-ethyl-1-(N-linolenoylamino)ethyl
3-(N-(2,2,5.5-tetramethyl-1.3
1-dioxane-4-carbonyl)amino]propionate 2-isopropyl-2- (N- (2-isobrobylhebutadecanoyl)amino]ethyl 3-[N(2.2
．． 5.5-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-isobutyl-2
-'(N-(2-ethyloctadecanoyl)amino]ethyl 3-[N-(2.2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]
Propionate 2.2-Pentamethylene-2-(N-linoleoylamino)ethyl 3-[N-(2,2.5.5-tetramethyl-1,3-dioxane-4-carbonyl)ami10
9] Probionate 2-phenyl-2-(N-linoleoylamino)ethyl 3-(N-(2.2.5.5-tetramethyl-1,
3-Dioxane-4-carbonyl)amino]propionate 2-benzyl-2-(N-linolenoylamino)ethyl 3- (N-(2.2.5.5-tetramethyl-1,
3-Dioxane-4-carbonyl)amino]propionate 2-naphthyl-2- (N- (2,2-dimethyl-
9-tetradecenoyl)amino]ethyl 3-[N-
(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 2-(2-
Furyl-2-(N-(2,2-dimethyl-9-octadecenoyl)amino)ethyl 3-(N-(2
．． 2.5.5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propionate 2-cyclopentyl-2-(N-(2,2-dimethyl-9-octadecenoyl)amino]ethyl 3-(N-(2.
2.5.5-tetramethyl-1,3-dioki 1 1 0 san-4-carbonyl)amino]propionate 2-(
3-indolyl)methyl-2-(N-linoleoylamino)ethyl 3-(N-(2,2,5.5tetramethyl-1,3-dioxane-4-carbonyl)amino)
Propionate 2-(8-heptadecenylcarbamoylamino)cyclohexan-1-yl 2- (N-(2,2,5.5-
tetramethyl-1,3-dioxane-4-carbonyl)
amino]acetate 2-(1-methyl-8-heptadecenylcarbamoylamino)cyclohexan-1-yl 4(N - (2.
2,5,5-tetramethyl-1,3-dioxane-4-
carbonyl)amino]butyrate 2-(1-methyl-8
-hebutadecenylcarbamoylamino)cyclohexan-1-yl 5(N-(2,2,5.5-tetramethyl-1.3-dioxane-4-carponyl)amino)
Valerate The compound of the present invention contains at least one asymmetric carbon atom, as shown by the * mark in the general formula (I), and is either an optically active form (R-unit or S-form) or a racemic form. It also includes forms.

The compound of the present invention has, for example, the following formula: A compound represented by the following formula R''-COZ' (Ml) or R'-NGO (IV) In the formula, zl is a hydroxyl group HC7l, a halogen atom such as Br; an alkoxy group such as methoxy, ethoxy; phenoxy, p −
Represents a substituted or unsubstituted phenyloxy group such as nitrophenoxy, 2,4-dinitrophenoxy; R3 and R4 are as defined above, or (b) reacts with a compound represented by the following formula: , R".R", n and Z1 are as defined above. and, if necessary, (c) the following formula 1 1 3 171 IQ oR! ＋ What? R3, A, X, Y and n are as defined above. It can be produced by removing the hydroxyl protecting group from a compound represented by the following.

The reaction of the compound of formula (n) with the compound of formula (I [[) in method (a) and the reaction of the compound of formula (V) with the compound of formula (Vl) in method (b) is usually In a suitable solvent, for example, aromatic hydrocarbons such as benzene, toluene, xylene; ethyl ether, tetrahydrofuran,
Ethers such as dioxane; esters such as methyl acetate and ethyl acetate; halogenated hydrocarbons such as methylene chloride, chloroform, and carbon tetrachloride; dimethylformamide,
High-boiling polar solvents such as dimethyl sulfoxide; Alcohols such as methanol and ethanol; Single or single solvents such as water
1 4 can be carried out in a mixed solvent. This reaction is generally −
From 78°C to the boiling point temperature of the solvent used, preferably about -10°C
It can be carried out within the range of the boiling point temperature of the solvent used.

Moreover, in method +a) and method (b), a catalyst or a reaction promoter can also be used in the reaction. Catalysts or reaction promoters that can be used include, for example, dicyclohexylcarbodiimide, diisobutylcarbodiimide, l-ethyl-3-(3-dimethylaminopropyl)
Carbodiimide compounds such as monocarbodiimide hydrochloride; acid anhydrides such as acetic anhydride and benzoic anhydride; sodium hydroxide;
Examples include inorganic bases such as potassium hydroxide, sodium carbonate, and potassium carbonate; organic bases such as triethylamine, diethylamine, dimethylamine, diisopropylamine, and pyridine.

These catalysts or reaction promoters are used in an amount of 0.01 to 10 equivalents, preferably 0.01 to 10 equivalents, based on compound (U) or compound (IV). It can be used within the range of 1 to 1.1 equivalents.

In addition, the ratio of compound (nl) or (IV) to compound (II) is not strictly limited, but compound (I[[) or (IV) is usually used per 1 mole of compound (■). 0.8-1.2 mol, preferably 1.0-1.
It can be used within the range of 1 mol.

Similarly, compound (V) is usually 0.8 to 1.2 mol, preferably 1.0 to 1.1 mol, per 1 mol of compound (Vl).
It can be used within a molar range.

In method (C), the reaction of removing the hydroxyl protecting group from compound (1-1>) can be carried out by hydrolysis in a solvent in the presence of an appropriate catalyst. For example,
Aromatic hydrocarbons such as benzene, toluene, xylene;
Ethers such as ethylene ether, tetrahydrofuran, and dioxane; Esters such as methyl acetate and ethyl acetate; Halogenated hydrocarbons such as methylene chloride, chloroform, and carbon tetrachloride; High-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol; Water; Organic acids such as acetic acid and propionic acid; Ketones such as acetone and methyl ethyl chloride alone or in a mixed solvent from -78°C to the boiling point of the solvent used, preferably about - It can be carried out within the range of 10° C. to the boiling point temperature of the solvent used. Catalysts that can be used include inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, and potassium carbonate; organic bases such as triethylamine, diethylamine, dimethylamine, diisopropylamine, and pyridine; hydrochloric acid, nitric acid, sulfuric acid, etc. Examples include mineral acids; hydrogen halides such as hydrogen fusodide, hydrogen bromide, and hydrogen iodide; and organic acids such as trifluoroacetic acid and trichloroacetic acid. Furthermore, the protecting group can be removed by catalytic hydrogenation using a suitable metal catalyst according to a conventional method.

As the metal catalyst that can be used in this case, common hydrogenation catalysts such as Nisokel, palladium, rhodium, platinum, etc. are used.

The products obtained by each of the above methods can be separated or purified from the reaction mixture by using a suitable combination of methods known per se, such as crystallization, chromatographic extraction, filtration, etc. .

1 1 7 Formula (V) used as starting material in the above method
, (II) and (Vl) can be produced as described below.

[Production of compound of formula (V)]

Process earth El (■ a) + Ph-CH. L 1 1 8 El upper (■ b) R" 0 OR21 zo (■ C) RI IQ o+p! Se (■ d) RI Io OR!+ and Yujth LL (V1a) 11111→ (■1d) In the above formula,
M is a hydrogen atom; represents an alkali metal atom such as sodium or potassium or an alkaline earth metal atom such as magnesium or calcium; L is OH, Cj2, Br,
represents I or N2, and R1R'', n and Z1 are as defined above.

Step 1 In this step, bantoyl lactone and ω-aminocarboxylic acid are reacted to synthesize compound (V 1a ). Vantoylactone is (D) (L) and (D
L) Either one may be used. Examples of ω-aminocarboxylic acids include aminoacetic acid (glycine), 3-aminoprobionic acid (β-alanine), 4-aminobutyric acid (γ-
Examples include aminobutyric acid, GAB^), 5-aminovaleric acid, and the like.

The reaction is preferably carried out using a solvent, such as aromatic hydrocarbons such as benzene, toluene, and xylene; ethers such as ethyl ether, tetrahydrofuran, and dioxane; high-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol; water can be used alone or in combination. This reaction can generally be carried out at a temperature within the range of about θ° C. to the boiling point of the solvent used, preferably from room temperature to the boiling point of the solvent used. It is preferable to use a catalyst for this reaction, and such catalysts include inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate; triethylamine, diethylamine,
Examples include organic bases such as dimethylamine, diisopropylamine, and pyridine. These catalysts have 0.0% relative to bantoyl lactone. Ol~10 equivalents, preferably 0.1~
It can be used within the range of 1.1 equivalent.

Step 1± This step is to convert compound (V-a) synthesized in Step 1 into compound (v-b) by benzylation.

As the reagent for benzylation, benzyl halides such as benzyl chloride, benzyl bromide, and benzyl iodide; benzyl alcohol; and phe-121-nyldiazomethane are used. This reaction is carried out in a suitable solvent, for example, aromatic hydrocarbons such as benzene, toluene and xylene; ethers such as ethyl ether, tetrahydrofuran and dioxane; esters such as methyl acetate and ethyl acetate; methylene chloride, chloroform, etc. In a single or mixed solvent such as halogenated hydrocarbons such as carbon tetrachloride; high boiling point polar solvents such as dimethylformamide and dimethyl sulfoxide; alcohols such as methanol and ethanol; ketones such as acetone and methyl ethyl ketone; It can be carried out usually at a temperature within the range of -78°C to the boiling point temperature of the solvent used, preferably -10°C to the boiling point temperature of the solvent used. Moreover, a catalyst or a reaction promoter can also be used in this reaction. Such catalysts or reaction promoters include, for example, dicyclohexylcarbodiimide, diisopropylcarbodiimide, 1-ethyl-3
= Carbodiimides such as (3-dimethylaminopropyl) monocarbodiimide hydrochloride Acid anhydrides such as acetic anhydride and benzoic anhydride; Sodium hydroxide, water 1 22 Inorganic bases such as potassium oxide, sodium carbonate, potassium carbonate; Triethylamine , diethylamine, dimethylamine, diisopropylamine, pyridine, and other organic bases. These catalysts or reaction promoters can be used in an amount of 0.01 to 10 equivalents, preferably 0.1 to 1.1 equivalents, based on compound (V1a).

Process 1 - This step is performed by converting the compound synthesized in the previous step 2 (v-
This is a step of protecting the hydroxyl group of b) to synthesize compound (Vc). Reaction reagents for introducing the protecting group (RI I . R 2 1 ) include, for example, acid anhydrides such as acetic anhydride and benzoic anhydride; acid chlorides such as acetyl chloride and benzoyl chloride; acetic acid, benzoic acid, p Organic acids such as toluenesulfonic acid; orthoesters such as ethyl orthoformate and methyl orthoformate; ketones such as acetone and cyclohexanone; aldehydes such as benzaldehyde and acetaldehyde; silylating agents such as trimethylsilyl chloride and dimethylphenylsilyl chloride; Alkylating agents such as diazomethane and dimethyl sulfate; alkyl halides such as methyl iodide and benzyl chloride are used. This reaction is carried out in a suitable solvent, for example, aromatic hydrocarbons such as benzene, toluene, xylene; ethers of ethyl ether, tetrahydrofuran, dioxane; methyl acetate,
Esters such as ethyl acetate; halogenated hydrocarbons such as methylene chloride, chloroform, and carbon tetrachloride; high-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; alcohols such as methanol and ethanol; ketones such as acetone and methyl ethyl ketone. ; in a single or mixed solvent such as water, from -78°C to the boiling point temperature of the solvent used;
Preferably, it can be carried out at a temperature within the range of about -10°C to the boiling point temperature of the solvent used. Moreover, a catalyst or a reaction promoter can also be used in this reaction. Such catalysts or reaction promoters include, for example, carbodiimides such as dicyclohexyllupodiimide, diisopropylcarbodiimide, 1-ethyl-3-(3-dimethylaminopropyl)monocarbodiimide hydrochloride; acetic anhydride, benzoic anhydride; Acid anhydrides such as acids; inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate;
triethylamine, diethylamine, dimethylamine,
Organic bases such as diisobutyramine and pyridine; organic acids such as acetic acid, p-toluenesulfonic acid and camphorsulfonic acid. These catalysts or reaction promoters can be used in an amount of 0.01 to 10 equivalents, preferably 0.1 to 1.1 equivalents, based on compound (v-b).

In this step, compound (V-c)' is converted into compound (V-d) by hydrolysis or catalytic hydrogenation.

This reaction can be carried out in a solvent using a suitable catalyst. Hydrolysis can be carried out, for example, by aromatic hydrocarbons such as benzene, toluene, and xylene; ethers such as ethyl ether, tetrahydrofuran, and dioxane; esters such as methyl acetate and ethyl acetate; Halogenated hydrocarbons; dimethyl 1
2 5 Polyhydric boiling point polar solvents such as formamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol; Water; Spinal acids such as acetic acid and propionic acid; Ketones such as acetone and methyl ethyl ketone, alone or in a mixed solvent.
78°C to the boiling point temperature of the solvent used, preferably about -10°C
The reaction can be carried out at a temperature within the range of from to the boiling point temperature of the solvent used. Examples of catalysts that can be used include inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, and potassium carbonate; triethylamine, diethylamine,
Organic bases such as dimethylamine, diisopropylamine, and pyridine; Mineral acids such as hydrochloric acid, nitric acid, and sulfuric acid; Hydrogen halides such as hydrogen fluoride, hydrogen bromide, and hydrogen iodide; Trifluoroacetic acid, trichloroacetic acid, etc. Examples include organic acids.

On the other hand, catalytic hydrogenation can be carried out by a conventional method known per se, and nickel, palladium, rhodium, platinum, etc. are used as the metal catalyst.

1 26 This is the process of converting. Reagents used in this reaction include halogenating reagents such as thionyl chloride, phosphorus oxychloride, and phosphorus pentachloride; alcohols such as methanol and ethanol; p-nitrophenol, 2.4-
Esterification reagents such as phenols such as dinitrophenol are used.

This step is carried out in a suitable solvent, for example, aromatic hydrocarbons such as benzene, toluene, xylene; ethers such as ethyl ether, tetrahydrofuran, dioxane; esters such as methyl acetate, ethyl acetate; methylene chloride, Halogenated hydrocarbons such as chloroform and carbon tetrachloride; High-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol;
The reaction can be carried out in a single or mixed solvent such as water at a temperature ranging from -78°C to the boiling point of the solvent used, preferably from about -10°C to the boiling point of the solvent used. It is also possible to use a catalyst or a reaction promoter for the reaction. Such catalysts or reaction promoters include carbodiimides such as dicyclohexylcarbodiimide, diisopropylcarbodiimide, and 1-ethyl-3(3-dimethylaminopropyl)monocarbodiimide hydrochloride; acids such as acetic anhydride and benzoic anhydride; Anhydrides; inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, and potassium carbonate; organic bases such as triethylamine, diethylamine, dimethylamine, diisobutyramine, and pyridine. These catalysts or reaction promoters are compounds (V-d
) 0.01 to IO equivalent, preferably 0.1 to 1
．． It can be used within the range of 1 equivalent.

This step is a step of synthesizing compound (■d) from compound (V-a). Examples of reagents that can be reacted with compound (V-a) include anhydrides such as acetic anhydride and benzoic anhydride; acid chlorides such as acetyl chloride and benzoyl chloride; and organic compounds such as acetic acid, benzoic acid, and p-luenesulfonic acid. Acids; Orthoesters such as ethyl orthoformate and methyl orthoformate; Ketones such as acetone and cyclohexanone; Benzaldehyde,
Aldehydes such as acetaldehyde; silylating agents such as trimethylsilyl chloride and dimethylphenylsilyl chloride; alkylating agents such as diazomethane and dimethyl sulfate;
Alkyl halides such as methyl iodide and benzyl chloride are used. This reaction can be carried out in a suitable solvent, e.g.
Aromatic hydrocarbons such as benzene, toluene, xylene;
Ethers such as ethyl ether, tetrahydrofuran, and dioxane; Esters such as methyl acetate and ethyl acetate;
Halogenated hydrocarbons such as methylene chloride, chloroform, and carbon tetrachloride; High-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol; Ketones such as acetone and methyl ethyl ketone; Water alone or -78℃ in mixed solvent
to the boiling point of the solvent used, preferably at a temperature within the range of about -10°C to the boiling point of the solvent used.

Moreover, a catalyst or a reaction promoter can also be used in this reaction. Such catalysts or reaction promoters include, for example, dicyclohexylcarbodiimide, diisopropylcarbodiimide, -ethyl-3
- Carposiimides such as (3-dimethylaminoprobyl) monocarbodiimide hydrochloride; acid anhydrides such as acetic anhydride and benzoic anhydride; inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate; Organic bases such as triethylamine, diethylamine, dimethylamine, diisopropylamine, pyridine; acetic acid, p-}
Examples include organic acids such as luenesulfonic acid and camphorsulfonic acid. These catalysts or reaction promoters are used in an amount of 0.01 to 10 equivalents, preferably 0.01 to 10 equivalents based on compound (v-b).
．． It can be used within the range of 1 to 1.1 equivalents.

Production of compound of formula (n)] Compound (II) is produced as described above in the following formula, where R'I n and Zl are 1 3 0 as defined above. It can be obtained by reacting the compound shown with the compound shown by the following formula (■) X-81YH (■) in which A.X and Y are as defined above.

This reaction is carried out in an appropriate solvent, such as aromatic hydrocarbons such as benzene, toluene, and xylene; ethers such as ethyl ether, tetrahydrofuran, and dioxane; esters such as methyl acetate and ethyl acetate; methylene chloride, chloroform, Halogenated hydrocarbons such as carbon tetrachloride; High-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol;
The reaction can be carried out in a single or mixed solvent such as water at a temperature ranging from -78°C to the boiling point of the solvent used, preferably from about -10°C to the boiling point of the solvent used. It is also possible to use a catalyst or a reaction promoter for the reaction. Such catalysts or reaction promoters include, for example, dicyclohexylcarbodiimide, diisopropylcarbodiimide,
Carbodiimides such as 1-ethyl-3-(3-dimethylaminopropyl)monocarbodiimide hydrochloride; halogenating reagents such as thionyl chloride, phosphorus oxychloride, and phosphorus pentachloride; acid anhydrides such as acetic anhydride and benzoic anhydride Inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate; Organic bases such as triethylamine, diethylamine, dimethylamine, diisopropylamine, pyridine; Acetic acid, p-toluenesulfonic acid, camphorsulfone Examples include organic acids such as acids. These catalysts or reaction promoters are 0.01 to 0.01 to compound (V).
It can be used in an amount of 10 equivalents, preferably 0.1 to 1.1 equivalents.

[Production of compound of formula (Vl)] Compound (VI) has the following formula HX - A - YH (
■) In the formula, A. X and Y are as defined above, and the compound represented by the following formula R"-Co-Z' (Vl)
In the formula, R3 and Z1 are as defined above.

This reaction is carried out in an appropriate solvent, such as aromatic hydrocarbons such as benzene, toluene, and xylene; ethers such as ethyl ether, tetrahydrofuran, and dioxane; esters such as methyl acetate and ethyl acetate; methylene chloride, chloroform, Halogenated hydrocarbons such as carbon tetrachloride; High-boiling polar solvents such as dimethylformamide and dimethyl sulfoxide; Alcohols such as methanol and ethanol;
The reaction can be carried out in a single or mixed solvent such as water at a temperature ranging from -78°C to the boiling point of the solvent used, preferably from about -10°C to the boiling point of the solvent used. It is also possible to use a catalyst or a reaction promoter for the reaction. Such catalysts or reaction promoters include, for example, dicyclohexylcarbodiimide, diisobutylcarbodiimide, 1-ethyl-3
-Carbodiimides such as (3-dimethylaminopropyl) monocarbodiimide hydrochloride; halogenating reagents such as thionyl chloride, phosphorus oxychloride, and phosphorus pentachloride; acid anhydrides such as acetic anhydride and benzoic anhydride; sodium hydroxide , inorganic bases such as potassium hydroxide, sodium carbonate, potassium carbonate; organic bases such as triethylamine, diethylamine, dimethylamine, diisobrobylamine, pyridine;
Examples include organic acids such as acetic acid, p-toluenesulfonic acid, and camphorsulfonic acid. These catalysts or reaction promoters can be used in an amount of 0.01 to 10 equivalents, preferably 0.1 to 1.1 equivalents, relative to compound (V).

The compound of formula (1) provided by the present invention has excellent ACAT inhibitory activity, and can be used for the treatment, treatment, etc. of hyperlipidemia, arteriosclerosis, angina pectoris, myocardial infarction, thrombosis, etc. It is expected to be used as a preventive drug.

The 80AT inhibitory activity of the compounds of the present invention is described below.
34 Can be confirmed by test method.

The ACAT inhibition test was performed using the method of Helgerud et al.
our own Lipid Research,
22, 497 (1981)] and the method of Folch et al. (Journal of Biological
Chemi-s try. 226. 497 (1
[1-140] Oleoyl Co
This was done by measuring cholesteryl oleate produced by A and intracellular cholesterol.

That is, 2 μM bovine serum albumin and 2 μM (1-1 A
C) 0.5 solution of oleoyl-CoA dissolved in 0.514 M potassium phosphate buffer (pF17.4)
mA', the microsomal fraction prepared from rat liver (
10 μl of a solution of 0.3 mg protein) dissolved in 0.514 M potassium phosphate buffer (pFl7.4) and test drug 1
5 μl of a solution of 0-7M dissolved in dimethyl sulfoxide
and react at 37°C for 4 minutes.

After that, methanol 4.2 lees! and chloroform 8.3
ml was added to stop the reaction, 2.5 m# of water was added, and after thorough shaking, the chloroform layer was separated. After concentrating the chloroform layer, it is subjected to thin layer chromatography, the produced cholesteryl oleate is fractionated, and the radioactivity is measured using a liquid scintillation counter.

Furthermore, the ACAT inhibitory activity of each test compound is calculated based on the radioactivity of a control obtained by performing the same test as above without using a specimen.

The results are shown in Table 1 below.

1 4 1 1 4 2 1 45 1 46 1 49 1 5 0 1 5 3 1 5 4 1 5 7 1 58 1 6 1 1 6 2 1 65 1 66 Hyperlipidemia and arteriosclerosis using the compound of the present invention as a drug When used for the treatment, treatment, prevention, etc. of diseases such as angina pectoris, myocardial infarction, and thrombosis, the compound may be used in combination with pharmaceutical auxiliaries such as pharmaceutically acceptable carriers, diluents, excipients, etc. binder, disintegrant,
Dosage forms suitable for administration, such as tablets, capsules, powders, etc., as well as lubricants, preservatives, stabilizers, solubilizers, flavoring agents, etc.
It can be formulated into unit dosage forms such as granules, microcapsules, syrups, elixirs, injections, and suppositories.

The content of the active ingredient in these preparations can vary widely depending on the type of compound of the present invention, the type of preparation, the purpose of use, etc., but is generally 0.5 to 90% by weight.
, preferably within the range of 5 to 60% by weight.

In solid preparations such as tablets, capsules, powders, and granules, the compounds of the present invention may be combined with lactose, mannitol, glucose, hydroxyprobylcellulose, microcrystalline cellulose, carboxymethylcellulose, starch, polyvinylpyrrolidone, metacalcinol, etc. Carriers or diluents such as aluminum acid and talc; lubricants such as magnesium stearate; disintegrants such as cellulose calcium gluconate; glutamic acid,
It can be formulated according to a conventional method together with a solubilizing agent such as aspartic acid and a stabilizer such as lactose. Furthermore, tablets may be coated with gastric or enteric substances such as sucrose, gelatin, hydroxypropyl cellulose, hydroxypropyl methylcellulose, etc., and capsules may be hard capsules or soft capsules. You may also do so.

In the case of liquid preparations such as syrups, elixirs, solutions, emulsions, suspensions, etc., the compounds of the invention may be mixed in a pharmaceutically acceptable liquid medium, such as purified water, saline, It can be formulated into a formulation by dissolving or dispersing it in a buffer, ethanol, etc., and further adding a surfactant, a sweetener, a flavoring agent, an aromatic agent, and a preservative sugar, if necessary.

On the other hand, injections for parenteral administration include sterile aqueous or non-aqueous solutions, suspensions, and emulsions. Such injections are prepared by mixing the compound of the present invention with an aqueous diluent such as distilled water for injection or physiological saline, or a non-aqueous diluent such as polyethylene glycol, propylene glycol, olive oil, ethanol, polysorbate 80 (registered trademark), etc. It can be prepared by Furthermore, injectables may contain preservatives, wetting agents, surfactants, dispersants,
Auxiliary agents such as stabilizers and solubilizing agents may also be included.

These injections can usually be sterilized by filtration using a bacteria-retaining filter, compounding with a bactericide, or irradiation, and after these treatments, they can be made into solid preparations by freeze-drying or other methods. Sterile water or a sterile injectable diluent may be added immediately before use.

The compounds of the present invention can be administered orally or rectally, or parenterally, such as intravenously, intramuscularly, subcutaneously. The dosage can vary depending on the type of compound used, the method of administration, the severity of the patient's symptoms to be treated, the age and weight of the patient, the doctor's judgment, etc., but in general, it is 1 to 6 times a day. 9. Approximately 2 to 500 mg/kg body weight once or twice a day
It is appropriate to administer the drug in four divided doses. However, the above-mentioned dosage range is only a tentative guideline, and it is of course possible to administer an amount above or below the above-mentioned range depending on the judgment of the doctor, the severity of the symptoms, etc.

Hereinafter, the present invention will be explained in more detail with reference to Examples.

Reference example-1 0-oleoylaminoaniline oleic acid 2. 82 g and 0-phenylenediamine 1. 6 2 g and 50 lIII of methylene chloride! ．． N,N'-dicyclohexylcarbodiimide 2. 27 g was added and stirred at room temperature overnight.

After the reaction, the insoluble matter was filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography at 170° C. to obtain 2.84 g of the title compound (yield: 76%).
) was obtained.

Properties: Oily I R (cm-', neat); νsu3284
, νco1646 mass spectrometry Molecular formula; C24H4. N2
0 Theoretical value 372.3140 Actual value 372.3129 NMR (δ, CDCj2 3); 0.88 (3H,
t, J=7Hz), 1.181.45(20H, m
), 1.65-1.81 (2H, m), 1.90-2.
09 (4H, m), 2.41 (20, t, J=7Hz
), 3.84 (2H, brs), 5.28-5.4
3 (2B, m), 6.76-6.83 (2Lm), 7
．． 02-7.13 (2N, m), 7.17 (1B, d,
J=8Hz) 2 m-oleoylaminoaniline 1. 62 g of N,N'-dicyclohexyllupodiimide were dissolved in 50 mj2 of methylene chloride, and while stirring under water cooling, 2.2 g of N,N'-dicyclohexyllupodiimide was dissolved. 27 g was added and stirred at room temperature overnight.

After the reaction was completed, insoluble materials were filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain 2.60 g (yield: 70%) of the title compound.

Properties: Oily I R (cm-', neat); v 8833
24, νcol658 mass spectrometry molecular formula; C24H4
. N20 theoretical value 372.3140 Actual value 372.3143 NMR (δ, CDCj2:+); 0.88 (3H,
t, J=7Hz), 1.201.42(20H, m
), 1.64-1.78 (20, m), 1.90-2.
09 (4H, m), 2.32 (2H, t, J=7Hz
), 3.70 (2B, brs), 5.29-5.40 (
2B, n+), 6.42 (1}1, d, J=8Hz
), 6. 62 (IH, d, J=8Hz),
7.00 (1B, brs), 7.21 (1B, s)
3 p-oleoylaminoaniline oleic acid2. 8 2 8 and p-phenylenediamine 1. 62 g of N,N'-dicyclohexylcarbodiimide was dissolved in 50 mj2 of methylene chloride, and while stirring under water cooling, 2.2 g of N,N'-dicyclohexylcarbodiimide was dissolved. 27 g was added and stirred at room temperature overnight.

After the reaction was completed, insoluble materials were filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain 2.85 g (yield: 77%) of the title compound.

Properties: Oily IR (cn+-', neat); v 81+32
94, V col656 mass spectrometry molecular formula; Cz4H
4oNzO theoretical value 372.3140 Actual value 372.3138 NMR (δ, CDCI!.s); 0.88 (3H, t
, J=7Hz), 1.181 73 4 p 1.42 (20Lm), 1.64-1.77 (2H, m
), 1.92-2. Q9 (4H, m), 2.31
(2H, t, J=7Hz), 3. 60 (2H, b
rs), 5.29-5.40 (2Lm), 6.65
(2H.d, J=9Hz), 6.92 (1B, brs)
, 7.26 (2H, d.J=9Hz) Oleoylaminophenol OI Oleic acid 2. 8 2 g and p-aminophenol 1
．． 64g of N,N'-dicyclohexylcarbodiimide were dissolved in 50lIIl of methylene chloride, and while stirring under water cooling, 2. 27 g was added and stirred at room temperature overnight. After the reaction, insoluble matter was filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography.
1.57 g (yield 42%) of the title compound was obtained.

174? Oily IR (cm-', neat); I/Nll,
V col646 mass spectrometry molecular formula; C24H39N
O ■ Theoretical value 373. 2980 Actual value 373.2988 NMR (δ, CDCj23); 0.8B (3H, t,
J=7Hz), 1,201.42 (20H, m), 1
．． 65-1.79 (2H, n+), 1.89-2.09
(4H.m), 2.3H2■, t+ J=7H2)
, 5.28-5.41 (2H, m), 6.77 (2H
．． d, J=9Hz), 7.04 (LH.brs), 7.
32 (2■, d, J = 9 Hz) 5 2.4-Diacetoxy N- (3- ((4hydroxyphenyl)amino]-3-oxobutyl)-3.3-dimethylbutanamidomethyl-1-oxobutyl ) Amino]propionic acid 3. 0 3 g and p-aminophenol 2. 1
8 g of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride was dissolved in 50 mf of methylene chloride and stirred with water cooling. 30 g was added and stirred at room temperature overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The obtained residue was purified by silica gel column chromatography to obtain the title compound i. 92 g (yield 50%) was obtained.

Properties: Oily IR (cm-low, neat): νcal750,
1660 Mass spectrometry Molecular formula i C+ Jz6NzO7 Theoretical value 394.1740 Actual value 394. 1746 NMR (δ, CDCf3); 1.02 (38,
s), 1.06 (3H, s), 2.05 (3H, s),
2.07 (3H.s), 2.55 (2H, t, J=6
Hz), 3.55-3.71 (2H, n+), 3.8
4 (18, d, J = 12 Hz), 4.03 (IH, d
, J=12Hz), 4.90(IH,s), 6.74-
6.83 (IH, m), 6.79 (2H, d,
J=8Hz), 7.35 (2H, d, J=8Hz), 7
．． 47(18, brs) 6 S-4-aminophenyl 3- (N- (2.4
-diacetoxy3.3-dimethyl-1-oxobutyl)amino]propanethionate 3- (N- (2.4
-Diacetoxy3.3-dimethyl-1-oxobutyl)amino]probionic acid1. 5 2 8 and p-aminothiophenol 1. 0 0 g and methylene chloride 50
1-ethyl-3 hydrochloric acid dissolved in mj2 and stirred with water cooling.
-(3-dimethylaminopropyl)carbodiimide2.
30 g was added and stirred at room temperature overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The obtained residue was subjected to silica gel column chromatography to obtain the title compound. It was purified by subjecting it to 335 g NMR graphy to obtain (yield: 16%).

Properties: Oily mass spectrometry molecular formula: C+ JzJzO6S Theoretical value 410. 1511 Actual value 410. 1520 (δ, CDCjL); 1.01 (3■+s), 1.
06 (31{.s), 2.06 (3H, s), 2.11
(3H, s), 2.87 (2H.t, J=6Hz), 3
．． 44-3.69 (2H, m), 3.81 (18, d
, J=11Hz) ,4.03(IH,d,J=11
Hz), 4.97 (IH, s), 6.50 (I
H, t, J=6Hz), 6.92(2■, d, J=
8 Hz), 7.24 (2H, d, J = 8 Hz) aminophenyl 9-octadecene 7 S-4 thioate 17 8 oleic acid 2. 82 g and p-aminothiophenol 1.88 g were dissolved in 50 mβ of methylene chloride, and N,N'-dicyclohexylcarbodiimide 2. 27 g was added and stirred at room temperature overnight.

After the reaction was completed, insoluble materials were filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain 2.86 g (yield: 74%) of the title compound.

Properties: Oily IR (cn+-', neat): V 81135
00, ν. ．． 1698 mass spectrometry molecule 2; C24H3
9NOS theoretical value 389. 2752 Actual value 389. 2754 NMR (δ, CDCffi 3); 0.88 (3
H. t. J=7Hz), 1.19-1.41 (20
H, m), 1.62-1.75 (2H, m), 1.9
1-2.09 (4H, m), 2.60 (2Fl, t,
J=7Hz), 3.83 (2H, brs), 5.29-
5.4N2■+m), 6.68(2■, d, J=8Hz
), 7. 16 (2H. d, J=8HZ)8
N-(4-hydroxyphenyl)-3-(N(2,2,
5.5-tetramethyl-1,3-dioxane 4 carbonyl)amino] propanamide 3- (N-(2,2,5.5-tetramethyl-1,3
-dioxane-4-carbonyl)amino]propionic acid 1. 0 4 g and p-aminophenol 0.665 g
and was dissolved in 30 mj2 of methylene chloride, and while stirring under water cooling,
Hydrochloric acid 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide 0. 96 g was added and stirred at room temperature overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The obtained residue was purified by silica gel column chromatography to obtain 1.37 g (yield: 98%) of the title compound.

Properties: Oily I R (cm-', neat); νcol66
0 Mass spectrometry molecular formula; C+sHzJzOs theoretical value 3
50. 1841 Actual value 350.18.46 NMR (δ, CDC l 3) i 0. 97 (
3H, s), 1.04 (3H, s), 1.41 (3
H, s), 1.45 (3H, s), 2.26 (2H,
t, J=6Hz), 3.50-3.72 (28, m)
, 3.28 (IH, d, J=12Hz> , 3.68
(LH.d, J=12Hz>, 4.10(18,s),
6.78 (2H.d, J=8Hz), 7.13 (1B,
t, J=6Hz), 7.32(2H, d, J=8H
z), 8.02 (IH, s) 9N-(4-hydroxyphenyl) -3- (N-
(2.2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino)propanamide 1 8 1 ]X 00 00 1- CN-(2,2,5.5-tetramethyl- 1.3
-dioxane-4-carbonyl)amino]probionic acid 1. 30 g and p-aminothiophenol 1. O
0.0 g of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride was dissolved in 30 ml of methylene chloride and stirred while cooling with water. 96 g was added and stirred at room temperature overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The obtained residue was purified by silica gel column chromatography to obtain 0.28 g (yield: 15%) of the title compound.

Properties: Oily IR (c+r', neat); v col692 mass spectrometry Molecular formula: C+llHzJz (las theoretical value
366.1613 Actual value 366.1608 1 82 NMR (δ, CDCj2 3); 1.00
(3H, s), 1.04 (3H, s), 1.42 (
3H, s), 1.45 (3B, s), 2.78-2.9
7 (2H, m), 3.29 (IH, d, J=1111z
), 3.453.71 (2H, m), 3.69 (I
H, d, J=11Hz), 4.08 (IH, s),
6.69 (2H, d, J=8Hz), 6,846.92
(IH, m), 7.15 (2H, d, J=8Hz)
0-oleoylaminophenol 10 0I 2-aminophenol 1. 0 9 g to 2 ethyl acetate
1.0 ml of sodium carbonate dissolved in a mixed solvent of 20 mj2 of water. 2.7 g of oleic acid chloride was added under water-cooling and stirring. 0 1 g of acetic acid 10mi! ．．
A solution dissolved in was added dropwise to the mixture, and the mixture was stirred as it was for 2 hours. After the reaction was completed, the organic layer was separated, washed with water and then with saturated brine, dried over anhydrous sodium sulfate, and the solvent was distilled off. Pour the resulting residue? Purified by mucochromatography to obtain 3.40 g of the title compound (yield: 9
1%).

Properties: oily IR (cm-', neat); v. ol64
6 Mass spectrometry Molecular formula i Cl+41{39NO■ Theoretical value 373.2980 Actual value 373.2988 NMR (δ, CDCIl3)i 0.8B(3H, t
, J=7Hz), 1.18-1.45 (208, m),
1.66-1.80 (2H, m), 1.92-2.10
(4H.m), 2.45 (2H.t.J=7Hz),
5. 28-5. 40 (2■.m), 6.85 (
2H, d, J = 8 Hz), 6.97 (IH, d, J = 8
Hz), 7.02 (IH, d, J=8Hz), 7.13
(18, t, J=8Hz), 7.45 (1■, br
s) 11 N-(2-hydroxyphenyl)-3(N
- (2,2,5.5-tetramethyl-1.3 dioxane-4-carbonyl)amino]propanamide s- (N-(2,2,5.5-tetramethyl-1,3
-dioxane-4-carbonyl)amino]prohyonic acid 0. 2 6 g and 0.13 g of 0-aminophenol in 10 mj of ethylene! Dissolved in hydrochloric acid while stirring with water cooling.
1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide 0. 20 g was added and stirred overnight at room temperature. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The obtained residue was purified by silica gel column chromatography to obtain 0.34 g (yield: 98%) of the title compound.

Properties: Oily I R (cn+-', neat); ! l. ．． 1
660 Mass spectrometry Molecular formula i C+aEli6NzOs Theoretical value 350.1841 Actual value 350. 1843 1 8 5 (δ, CDCI!.s); 0.97 (3H, s),
1.03 (3H, s), 1.42 (3H, s), 1.4
6 (3■+s), 2.77 (2H, t, J=6Hz)
, 3.28 (2■, d, J=12Hz) , 3.59
3.77 (2H, m), 4.11 (IH, s), 6.8
6 (IH, t, J=8Hz), 7.01 (IH, d,
J=8Hz), 7.08-7.22 (3H, m), 8.
80(1■+s)12 N-(2-aminophenyl)
-3-(N(2,2.5.5-tetramethyl-1.3-
Dioxane-4-carbonyl)amino]propanamide NMR 3 3 (N- (2.2.5.5-tetramethyl-1.dioxane-4-carbonyl)amino]pro1 8 6 Hyonic acid 3.8 9 g and 0 -phenylene diamine 2
．． 16g of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride was dissolved in 50ml of methylene chloride, and stirred while cooling with water. 88 g was added and stirred overnight at room temperature. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The obtained residue was purified by silica gel column chromatography to obtain the title compound 2. 48 g (yield 47%) was obtained.

Properties: Oily IR (cn+-', neat); v. ol66
0 Mass spectrometry Molecular formula i C+ 8H27N304 Theoretical value 349.2001 Actual value 349.1993 NMR (δ, CDCJ2 3)? 0.99 (3B,
s), 1.03 (3H, s), 1.42 (3H, s
), 1.46 (3H, s), 2.67 (2H, t+J
=6Hz), 3.59-3.70 (2■, m), 3.
28 (IH, d, J=12Hz), 3.68 (IH,
d, J=12Hz), 4.10 (IH.s), 6.72
-6.82 (2H, m), 7.037.16 (2H,
m), 7.20 (IH, d, J=8Hz), 13 7. 87 (1}1, s) m-linoleoylaminoaniline 0.841 g of linoleic acid and 0.0-phenylenediamine.
541g and 50mj of methylene chloride! N,N'-dicyclohexylcarbodiimide 1
．． 03 g was added thereto, and the mixture was stirred at room temperature overnight.

After the reaction was completed, insoluble materials were filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain 0.796 g (yield: 72%) of the title compound.

Properties: Oily I R (cm-', neat); v col6
46 Mass spectrometry Molecular formula; C24H311N20 theoretical value 370. 2984 Actual value 370.2981 NMR 14 (δ, CDCI!.3); 0.89 (3H, t, J=
7Hz), 1.22-1.43 (14H, m), 1
．． 63-1.88 (2H, m), 1.98-2.
11 (4H, m), 2.32 (2H, t, J=7H
z), 2.77 (2H, t, J=6Hz), 5.28
-5.46 (4H, m), 6.47 (IH, d, J
= 8Hz), 6.69 (LH, d, J = 811z), 7
．． 07 (IH, t, J=8Hz), 7.14 (1■+
s), 7.24 (2H.s) 342 mg of o-lauroylaminoaniline p-phenylenediamine was dissolved in 10 N of ethyl acetate.
1 of sodium carbonate dissolved in a mixed solvent of 10 nl of water and 10 nl of water.
Add 06 mg of lauric acid chloride 2 while stirring with water cooling.
A solution of 19 mg dissolved in 10 wl of ethyl acetate was added dropwise, and the mixture was stirred for 2 hours.

After the reaction is complete, separate the organic layer, add water and then add 18
9 Washed with saturated brine, dried over anhydrous sodium sulfate, and the solvent was distilled off. The obtained residue was purified by silica gel column chromatography to obtain 250 g of the title compound (
A yield of 86% was obtained.

Properties: Oily IR (cn+-', neat); v col65
1 Mass spectrometry Molecular formula i C+ 8HioNzO theoretical value
290.2358 Actual value 290.2362 NMR (δ, CDC jl! 3); 0.88 (3
■, t, J=7Hz), 1.17-1.42 (16H
, m), 1.63-1.78 (2■艷), 2.31 (
2H. t, J=7Hz), 3.581(2H, br
s), 6.64 (2H, d, J=9Hz), 6.
98 (1■, brs), 7.26 (2H, d, J
=9Hz) 15 p-linolenoylaminophenol OIJ 1 9 0 ? Nolenic acid 835mg and p-aminophenol 546m
N,N'-dicyclohexylcarpodiimide 61
8 mg was added and stirred at room temperature overnight. After the reaction was completed, insoluble materials were filtered, the solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain 1.03 g (yield: 55%) of the title compound.

Properties: Oily IR (cm”, neat); νCO1646 mass spectrometry Molecular formula: GtaHssNO■ Theoretical value 369.
2667 Actual value 369.2672 NMR (δ, CDCj2+); 0.97 (3■, t.
J=7Hz), 1.191.44 (8H, m), 1
．． 564.77 (2H, m), 1.98-2.12 (4
8, m), 2.33 (2H, t, J=7Hz), 2.
71-2.88 (4B, m), 5.26-5.45 (
6H. m), 6.77 (2H, d, J=9■2), 7.
05 (IH, s), 7.31 (2■, d.J=9Hz) 1 6 trans -2 - (oleoyleamino)cyclohexylamine (trans) trans - 1 . 1.14 g of 2-diaminocyclohexane and methyl oleate2. 9 6 g and benzene 15III! ．． Dissolve in sodium methoxide 0. 60 g was added and heated under reflux for 20 hours. After the reaction was completed, the solvent was distilled off under reduced pressure, the residue was dissolved in ethyl acetate and water, and the organic layer was separated. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate, and then the solvent was distilled off. The residue was purified by silica gel column chromatography to obtain the title compound 2. 5 4 g (yield 6
8%).

Properties: Oily mass spectrometry Molecular formula: CzaHabNzO theoretical value 37
8.3610 Actual value 378.3611 NMR (δ, CDCj23); 0.8B (3Fl,
t, J=7Hz), 1.121.48 (248, m)
, 1.53-1.79 (4H, m) , 1.91 (6
H, m), 2.18-2.35 (2■, m), 2.
52-2.95 (3H.m), 3.62-3.78
(IH, m), 5.28-5.40 (21LII1)
, 6.08-6.20 (IH, m) 17 (S,
S)-2-(oleoylamino)cyclohexylamine ■ (S,S)-1.2-diaminocyclohexane 1. 1
4 g and 2. methyl oleate. Dissolve 96 g of sodium methoxide in 15ij2 of benzene and add 0.6 g of sodium methoxide.
0 g was added and heated under reflux for 20 hours. After the reaction was completed, the solvent was distilled off under reduced pressure, the residue was dissolved in ethyl acetate and water, and the organic layer was separated. The organic layer was washed with saturated brine, dried over anhydrous flowing sodium, and then the solvent was distilled off. The residue was purified by silica gel column chromatography,
Title compound 2. 41 g193 (yield 65%) was obtained.

Properties: Oily mass spectrometry Molecular formula: CtaHabNzO theoretical value 37
8.3610 Actual value 378.3612 NMR (δ, CDCj! !!); 0.88 (3H,
t, J=7Hz), 1.12-1. 48 (24
H, m), 1.53-1.79 (4FI, m), 1
．． 91 (6H, m), 2.18-2.35 (2+1, m
), 2.52-2.95 (3H, m), 3.62-
3.78 (IH, +n), 5.28-5.40 (28,
m), 6.08-6.20 (IH, m)18 (
IR,2R)-2-(oleoylamino)cyclohexanol (IR,2R)-2-aminocyclohexanol1.
15 g to 10 mn of ethyl acetate and IOIII! of water!
．． 3.0 g of oleic acid chloride dissolved in water and stirred in water.
A solution prepared by dissolving 20 mffi of ethyl acetate was added dropwise, and after the dropwise addition was completed, the mixture was stirred for 3 hours. After the reaction was completed, the aqueous layer was removed, and the organic layer was washed with brine and dried over anhydrous sodium sulfate. The solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain the title compound 3.
．． 74 g (yield 99%) was obtained.

Properties: Oily mass spectrometry Molecular formula: CzaHasNOt theoretical value 37
9.3450 Actual value 379.3453 NMR (δ, CDCj23); 0.88 (3H, t,
J=7Hz), 1.10-1.42 (24H, m),
1.57-1.78 (48, m), 1.89-2.10
(6H, m), 2.22 (2H.t.J=7Hz>,
3.32 (IH, ddd, J=11Hz, 11Hz, 5
Hz), 3.583.70 (IH, m), 5.28-
5.50 (3H.m) 19 (Is, 23)-1-
(oleoylamino)cyclohexanol (Is,2S)-2-aminocyclohexanol 1.
15 g of ethyl acetate 10IIlj2 and water 10II
II! ．． To? Add oleic acid chloride 3 while cooling with water and stirring.
．． A solution of 0g dissolved in 20nl of ethyl acetate was added dropwise,
After the dropwise addition was completed, the mixture was stirred for 3 hours. After the reaction was completed, the aqueous layer was removed, and the organic layer was washed with brine and dried over anhydrous sodium sulfate. The solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain the title compound 3.7.
6 g (yield 99%) was obtained.

Properties: Oily mass spectrometry Molecular formula i C24H4SNO ■Theoretical value 37
9.3450 Actual value 379.3453 NMR (δ, CDCj!3)i0.88(3H,t,
J=7Hz), 1.101.42 (248, m), 1
．． 57-1.78 (4H.m), 1.89-2.10 (
6H, m), 2.22 (2H.t.J=7Hz), 3
．． 32 (IH, ddd, J=11Hz.11Hz.5H
z), 3,583.70 (IH, m), 5.28-5
．． 50(3H.m)20(IR,2R)-2-(
Stearoylamino)cyclohexanol (IR, 2R)-2-aminocyclohexanol 1.
15 g of ethyl acetate and 10 mj of water
Stearic acid chloride 3.0 is dissolved in
2g to 20ml of ethyl acetate! Drop the solution dissolved in
After the dropwise addition was completed, the mixture was stirred for 3 hours. After the reaction was completed, the aqueous layer was removed, and the organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain the title compound a.
．． og (100% yield) was obtained.

Properties; Oily mass spectrometry molecular formula; CzaH4JOz Theoretical value 381.3606 Actual value 381.3611 (δ, CDCj2 s); 0.8B (3L t, J
=7Hz), -1.41 (328, m), 1.57
-1.78 (4H, +n) NMR 1.11 1 9 7 1.89-2.11 (2H, m), 2.22 (2■
,t,J=7■2),3.31(IH,ddd,J=1
1Hz, 11■Z, 5FIz), 3.58-3.70(
IN, n+), 5.42-5.51 (1}1, m)
21 (Is,23)-2-(linoleoylamino)cyclohexanol ■ (Is.2S)-2-aminocyclohexanol 1.
15 g in 10 ml of ethyl acetate and 10 ml of water!
．． Dissolve 2.98% of linoleic acid chloride in water and stir with water cooling.
A solution of g dissolved in 20 mA of ethyl acetate was added dropwise, and after the dropwise addition was completed, the mixture was stirred for 3 hours. After the reaction was completed, the aqueous layer was removed, and the organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was distilled off, and the resulting residue was purified by silica gel column chromatography to obtain the title compound 3.7.
6 g (yield 100%) was obtained.

Properties: Oil mass spectrometry Molecular formula: CzJaJOz 1 9 8 NMR Theoretical value 377.3293 Actual value 377.3299 (δ, CDCj2s); 0.89 (3Fl.t, J4
Flz), 1.121.41 (18H, m),
1.58-1.77 (4H, m), 1.89-2.
18 (6H.m), 2.22 (2H.t, J=8H
z), 2.77 (2■+t+J=6Hz), 3.3
1 (2H, ddd, J=11Hz, 11Hz, 5H
z), 3.59-3. 70 (IN, m), 5.
29-5.47(51,+n) Example-1 N-(2-(oleoylamino)phenyl]-3-
(N- (2.2,5.5-tetramethyl-1.3-
dioxane-4-carbonyl)amino]propanamide H 372 mg of 2-aminooleoylanilide and 3(N-
259 mg of (2.2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]probionic acid was dissolved in 30n+42 methylene chloride, and 1-ethyl-3-(3-dimethyl hydrochloride) was dissolved under water cooling. 211 mg of (aminopropyl) carbodiimide was added thereto, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off.

Then, the residue was subjected to silica gel column chromatography to obtain 500 mg (yield: 82%) of the title compound.

Properties: Oil optical rotation [α) o; +29.0 (C=1.0,
CHCj2 3) I R (cm-', neat)
; v c-o 1664 mass spectrometry molecular formula; C36
H59N30S theoretical value 613.4454 actual value 613.4425 NMR (δ, CDCj23); 0.88 (3H, t,
J=7Hz), 0.98(3H.s), 1.04(3
8, s), 1.22-1.40 (20+1, m), 1.
42 (3Ls), 1.45 (3H,s), 1.62-1
．． 77 (2H, m), 1.94-2.09 (411.m
), 2.36 (2L t, J=7Hz), 2.6
0 (2H. t, J=6Hz), 3.28 (LH, d,
J=12Hz), 3.55-3.66(2H.lI
1), 3.69 (ILd, J=12Hz), 4.1
0 (1 fl.s), 5.29-5.42 (2B, m)
, 7.14-7.48 (2H, m) , 7.39-
7.48 (2H, +n), 8.18 (IH, s),
8.60 (IH, brs) Example-2 N- (2- (oleoyl ζ-no) phenyl]-3=
(N-(2,4-diacetoxy3.3-dimethyl-1-oxobutyl)amino)propanamide ■ 2 0 1 0-oleoylaminoaniline 744B and 3(N-
2.4-diacetoxy3.3-dimethyl-1-oxobutyl)amine propionic acid (600 mg) and methylene chloride (30, mj!). 442 mg of 1-ethyl-3-(3-dimethylaminopropyl)carpodiimide hydrochloride was added to the mixture under water-cooling and stirring, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off.

Then, the residue was subjected to silica gel column chromatography to obtain 810 mg (yield: 62%) of the title compound.

Properties: Oily optical rotation [α]. ; +6.30° (C=1.0, C
HCβ3)I R (cm-'+neat); νc
-o 1750+ 1660 mass spectrometry molecular formula; C3
? HS9N307 Theoretical value 657.4352 Actual value 657.4369 NMR (δ, CDCj!s); 0.8B (3H.t,
J=7Hz), 1.02(3H.s), 1.06(3
8, s), 1.23-1.45 (20H, m), 1.6
7-1.79 (2H, m), 1.95-2.09 (4
H, 20 2 m), 2. 03 (2H, s), 2.04 (3■+
s), 2.42 (2FI. t, J=7■2), 2.
58 (2■, t+J=6Hz), 3.49-3.7
2 (2H, m), 3.83 (211, d, J=11
Hz), 4.02 (IH, d, J=11Hz), 4
．． 89 (LH.s), 5.30-5.44 (2FI, m
), 6.72-6.81 (IH, m), 7.1
9-7.32 (211, m), 7.37 (IH.d
．． J=8Hz), 7.59 (ILd, J=8Hz), 7
．． 88 (ILbrs), 8.19 (IH.brs) Example-3 N-(2-(oleoylamino)phenyl]-3(
N-(2,4-dihydroxy-3,3-dimethyl-1-
oxobutyl)amino]propanamide N-(1- (oleoylamino)phenyl]-3(
N-(2,4-diacetoxy-3,3-dimethyl-1
470 mg of -oxobutyl)amino]propanamide was dissolved in 4 ml of methanol, and while stirring at room temperature, 1.51 I1 of an IN aqueous solution of caustic soda was added and the mixture was further stirred for 30 minutes. After the reaction is complete, add 10ml of water and add 20ml of methylene chloride.
l! Extracted with. The methylene chloride layer was washed with water and then with saturated brine, dried over anhydrous sodium sulfate, the solvent was distilled off, and the residue was subjected to silica gel column chromatography to obtain 377 mg (yield 94%) of the title compound. .

Properties; Oil optical rotation [α]; ÷21.9° (C・1.0, CHC
I! ．． 3) I R (cm-I.neat); νN
II+ νOll+ νc-o 1660 mass spectrometry molecular formula; C3JssNaOs theoretical value 573.41
41 Actual value 573.4146 NMR (δ, CDCj'+); 0.88 (3H, t,
J=7Hz), 0.90(38,s), 0.97(3
H, s), 1.20-1.42 (20H, II1), 1
．． 62-1.76 (2H, m), 1.94-2.01
(4B, m), 2.38 (2H, t, J=7Hz),
2.52 (2H, t, J=6Hz), 3.44 (2H,
s), 3.49-3.72 (28, m), 3.94
(IH, s), 5.28-5.42 (28, m),
7.137.21 (2B, n+), 7.29-7.
49 (3H.m), 8.31 (IH, s), 8.6
9(IH,s) Example-4 N-(2-(linoleoylamino)phenyl]-3
- (N- (2,2,5.5-tetramethyl-1,3
-dioxane-4-carbonyl)amino]propanamide N-(2-aminophenyl)-3- (N-(2.2,
3492.05 IIlg of 5,5-tetramethyl-1.3-dioxane (4-carbonyl)amino]propanamide, 280mg of linoleic acid and 227mg of dicyclohexyllupodiimide were dissolved in 15lIll of toluene and heated under reflux for 2 hours. After cooling the reaction solution, the resulting crystals were filtered, the filtrate was concentrated, and the residue was subjected to silica gel column chromatography to obtain 266 mg of the title compound (yield: 4
4%).

Properties; Oil optical rotation [α) D; +21.3° (C=1.
0,CHC23)I R (cm-', neat);
v co-o 1662 mass spectrometry molecular formula H C3Js
JaOs theoretical value 611.4298 Actual value 611.4264 NMR (δ, CDCI!.3); 0.89 (3H, t
, J=7Hz), 0.98(3H.s), 1.04(
3H, s), 1.23-1.44 (14H, +m), 1
．． 42 (3H, s), 1.45 (38, s), 1.65
1.77 (2■+m), 1.91-2.10 (4H, m
), 2.37 (2}1, t, J=7Hz), 2.
62 (2H, t, J=6Hz), 2. 77 (2H
, t. J=6H2), 3.28(IH.d, J=1
2Hz), 3.56-3.67 (2Lm), 3.69
(1}1, d, J=12Hz), 4.10 (IH.s)
, 5.29-5.44 (4H, n+) , 7.0920
6 (1tL t, J=6Hz), 7.15-7.22 (
2H, m), 7.42-7.49 (2H, m)
, 8.11 (LH, s), 8.55 (IH, s) Example-5 N-C2-(linoleoylamino)phenyl]3-
(N-(2,2,5.5-tetramethyl-1,3-dioisane-4-carbonyl)amino)propanamide N-(2-aminophenyl)-3- (N- (2,2
, 5,5-tetramethyl-1,3-dioxane 4-carbonyl)amino] 349 mg of propanamide, 278 mg of linolenic acid, and 227 mg of dicyclohexylcarbodiimide
mg was dissolved in 15 ml of toluene and heated under reflux for 2 hours. After cooling the reaction solution, the crystals formed were removed by filtration, and the filtrate was concentrated and subjected to silica gel column chromatography to obtain the title compound 271 (yield: 45%).

Properties; Oil optical rotation [α] n i +26.2 (C 1.0,
CHCffi3)IR (cm-', neat)
; pc-o 1660 mass spectrometry molecular formula; C36
FISSN3 0S theoretical value 609.4141 Actual value 609.4144 NMR (δ, CDCf 3); 0.97 (3H.
t, J=7Hz), 0.98(3}1,s), 1.
04 (3H, s), 1.23-1.43 (8H.m)
, 1.42 (3H, s), 1.46 (3}1, s),
1.65-1.77 (2H, m) + 2.03-2.
12 (4H, m) + 2.38 (2H.t, J = 7Hz
), 2.63 (2H.t, J=6Hz). 2.75
-2.83 (4H, m). 3.28 (IH.d, J=
12Hz), 3.58-3.70 (28, m). 3
．． 69 (1■, d, J=12Hz), 4.11 (LH
, s), 5.29-5.43 (6H.m). 7.09
(IH, t, J=6Hz), 7.17-7.22 (2H
,+n). 7.42-7.51 (2H, m), 8.0
6 (IH, brs), 8.51 (IH, brs) Example-6 N- [1- (stearoylamino) phenyl] 1-
[N-(2,2,5.5-tetramethyl-l.3-
dioxane-4-carbonyl)amino]propanamide N-(2-aminophenyl)-3- [N- (2.2
, 5.5-tetramethyl-1.3-dioxane 4-carbonyl)amino]propanamide (349 ml) was dissolved in 20 ml of methylene chloride, pyridine 1d was added while stirring under water cooling, and then 303 ml of stearic acid chloride was dissolved in 3 d of methylene chloride. The solution was added dropwise, and the mixture was further stirred for 1 hour. After the reaction was completed, the reaction solution was washed with water, dried with anhydrous sodium sulfate,
After distilling off the solvent 209, the residue was subjected to silica gel column chromatography to obtain the title compound 507 (yield: 82%).

Properties; Oil optical rotation [αL; +27.3 (C=1.0, CHC
ffii) IR (cm-', neat); v
c. o 1664 mass spectrometry molecular formula i C36H61N
3 0S theoretical value 615.4611 Actual value 615.4582 NMR (δ, CD (If! 3); 0.88 (3
H. t, J=7Hz), 0.98(38,s). 1
．． 04 (38, s). 1.20-1.43 (28H,
m), 1.43 (3■, s), 1.46 (31{, s
), 1.684.78 (28, m), 2.40 (2
H, t, J=7Hz), 2.65(2■, t, J=6
Hz), 3.28 (IH.d, J=12Hz). 3
．． 58-3.72 (2H, n+), 3.69 (IH,
d, J=12Hz). 4.11(LH,s). 7.
08 (IH, t, J=6Hz). 7.17-7.23
(2H, m), 7.42-7.53 (21+, m),
8.00 (1B, s), 8.49 (IH, s) Example-7 N-[1-(lauroylamino)phenyl]-32
1 0 - [N- (2.2,5.5-tetramethyl-1.3
-dioxane-4-carponyl)amino]propanamide N-(2-aminophenyl)-3-[N- (2,2,
5.5-Tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide (349 µm) was dissolved in 20 methylene chloride, and while stirring under water cooling, 1 part of pyridine was added, and then 219 µm of lauric acid chloride was dissolved in 3 parts of methylene chloride. wr
A solution dissolved in 1 liter of water was added dropwise to the mixture, and the mixture was further stirred for 1 hour. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain the title compound 454 (yield 86%).
) was obtained.

Properties: Oil optical rotation [α] o i +31.7 (C・1.0.
CHCj23)IR (cm-', neat)
; vc-o 1664 mass spectrometry molecular formula ica. Hn
JJ+ Os theoretical value 531.3672 Actual value 531.3692 NMR (δ, CDCj! 3); 0.8B (3H
, t, J=7Hz), 0.98 (3 ■s), 1.0
4 (3H, s), 1.21-1.43 (16H, m)
, 1.42 (3H, s), 1.45 (3H, s),
1.65-1.77 (2■, n+), 2.38 (2H
, t. J=7Hz), 2.6N2■,t, J=6Hz
), 3.28 (IH, d, J=12Hz), 3.5
5-3.68 (2B, n+), 3.69 (LH, d.
J=12Hz), 4.10(IH,s)17.09(
IH, t, J=12Hz). 7.14-7.22 (2
■, m), 7.40-7.49 (2H, m), 8.
13(IH,s), 8.57(IH,s) Example-8 N-[2-(octanoylamino)phenyl]3-
[N-(2,2.5.5-tetramethyl-1.3-
Dioxane-4-carbonyl)amino]brobanamide N-(2-aminophenyl) -3- [N- (2.
2,5.5-tetramethyl-1,3-dioxane = 4-
Carbonyl)amino]propanamide 349 is dissolved in methylene chloride 20, and pyridine lmj! is stirred under ice cooling.
Then, a solution of 163 μm of octanoyl chloride dissolved in 3 μm of methylene chloride was added dropwise, and the mixture was further stirred for 1 hour.

After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain the title compound 413■ (yield 87.
%) was obtained.

Properties; Oily 2 1 3 Optical rotation [α] D; +35.1 (C・1.0. CH
Cj2s)IR (cm-'+neat);
vc-o 1664 mass spectrometry molecular formula; (:26
H41N3 0S theoretical value 475.3046 Actual value 475.3039 NMR (δ, CDCj! 3); 0.89 (3H
．． t, J=7Hz), 0.98 (3H.s), 1
．． 04 (3H, s). 1.23-1.38 (8H, m
), 1.42 (3H, s), 1.45 (3H, s).
1.62-1.77 (2H, m). 2.37 (2H
．． t, J = 7Hz), 2.60 (2■, t, J = 6H
z), 3.28 (1■, d, J=12Hz). 3.
57-3.71 (2Lm). 3.69 (11, d.J.
=12Hz). 4.10(IH,s), 7.09(
IH. t. J=6Hz). 7.14-7.2N2■,
m), 7.40-7.49 (2H.m). 8.16
(IH, s). 8.59 (IH, s) Example-9 N-[3-(Linooylamino)phenyl]-3[
N-(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide 2 1 4 3-linoleoylaminoaniline 555■ and 3[N-
(2.2.5.5-tetramethyl-1.3-dioxane-4-carponyl)amino]propionic acid was dissolved in 30 parts of methylene chloride, and under water cooling, hydrochloric acid, 1-ethyl-3-( 316 II g of 3-dimethylaminopropyl)carbodiimide was added, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off.

The residue was then subjected to silica gel column chromatography to obtain the title compound 786 (yield: 86%).

Properties; Oil optical rotation [αL; +30.8 (C=1.0, CHC
J2s) IR (cm-', neat); v
c. o 1664 mass spectrometry molecular formula i CsaHsJ
30s theoretical value 611.4298 Actual value 611.4389 NMR (δ, CDC 1 3); 0.89 (3H
, t, J=7Hz), 0.96(31{,s),
1.03 (3H, s). 1.23-1.42 (14H
, n+), 1.41 (3H.s). 1.45 (38,
s), 1.62-1.78 (2H, m), 1.99
-2.08 (4H, m). 2.33 (2H, t, J=7
Hz), 2.64 (2H, t, J=6Hz), 2.7
7 (2H.t.J=6Hz), 3.26 (IFI, d,
J=12Hz). 3.52-3.73 (2H, m).
3.68 (IFl.d, J=12Hz), 4.11 (
IH, s), 5.295.43 (2H.m). 7.
09 (IH, t.J=6Hz), 7.22-7.29
(2H, m). 7.34-7.42 (2H, m),
7.79 (IH, s), 8.36 (IH, brs)
Example-10 N-[3-(oleoylamino)phenyl]-3[
N-(2,4-diacetoxy3,3-dimethyl-1
-oxobutyl)amino]propanamide m-oleoylaminoaniline 744■ and 3[N- (
2.4-diacetoxy3.3-dimethyl-1-oxobutyl)amino]propionic acid (606) was dissolved in methylene chloride (30Id), and under water cooling, 1-ethyl-3 hydrochloride was dissolved.
-(3-dimethylaminopropyl)carbodiimide 42
2■ was added, and the mixture was stirred overnight. Wash the reaction solution with water,
After drying over anhydrous sodium sulfate, the solvent was distilled off. Then, the residue was subjected to silica gel column chromatography to obtain the title compound 860.mu. (yield: 65%).

Properties; Oil optical rotation [α]D; ÷12. 8 (C・1.0.
CHCI! ．． s) IR (cm-', neat)
; l'(mQ 1750% 16682 1 7 Mass spectrometry molecule 2; C3JsJJ+ 07 theoretical value 6
57.4352 Actual value 657.4342 NMR (δ, CDCjL); 0.89 (3H, t,
J=7Hz). 1.03(38,s), 1.05(
3H,s). 1.21-1.42 (20H, m), 1
．． 61-1.77 (2H, m), 1.97-2.1
3 (4H, m). 2.05 (3H, s), 2.10 (
3H, s), 2.33 (2H, t, J=7Hz).
2.56 (2H, t, J=6Hz), 3.55-3.
68(2HIl1). 3.87 (IH, d, J=11
Hz), 4.02 (LH, d, J=10Hz). 4
．． 91 (IH, s), 5.29-5.42 (2H, m
). 6.84 (IH.d, J=6■Z), 7.25 (
LH, d, J = 8Hz). 7.33 (IH, d, J=8
Hz). 7.41 (In, d, J=8Hz), 7.5
4 (IH, brs), 7.63 (IH, brs),
8.01 (IH, brs) Example-11 N-[3-(oleoylamino)phenyl]-3-
[N-(2.4-dihydroxy-3.3-dimethyl-1-oxobutyl)aminocobrobanamide 2 1 8 N- [i (oleoylamino)phenyl] 3- [
N-(2,4-diacetoxy3,3-dimethyl-1
470 ml of -oxobutyl)amino]propanamide was dissolved in 4 ml of methanol, and while stirring at room temperature, 1.5 parts of IN aqueous sodium caustic solution was added, and the mixture was further stirred for 30 minutes. After the reaction was completed, 10 parts of water was added and the mixture was extracted with 20 parts of methylene chloride. The methylene chloride layer was washed with water and then with saturated brine, dried over anhydrous sodium sulfate, and after distilling off the solvent, the residue was subjected to silica gel column chromatography to obtain the title compound 378 (yield 94%). .

Properties; Oil optical rotation [α] n; +23.1 (C=1.0,
CHCI! ．． s)IR (cm-'+neat)
; vc-o 1660 mass spectrometry molecular formula i C+J
sslJa Os Theoretical value 573.4141 Actual value 573.4146 NMR (δ, CDCf! 3) i 0.88 (3H
, t, J=7Hz), 0.91 (311, s). 0
．． 98 (3H.s), 1.21-1.42 (20H,
n+), 1.62-1.73 (2H, m). 1.93
-2.10 (4H, m) 2.32 (2H, t, J=7H
z). 2.52 (2H brs). 3,503.7
0(2L m)+4.01(II,s). 5.29
-5.43 (2H, m), 7.17-7.31 (3H
, m). 7.53-7.62 (IH.m), 7.7
1 (18, brs), 7.92-8.00 (IH, m
). 8.46-8.55 (IN, m) Example-12 N-[4-(oleoylamino)phenyl]-3-
[N-(2,4-diacetoxy3,3-dimethyl-1-oxobutyl)amino]propanamide p-oleoylaminoaniline 744 ■ and 3[N- (
2.4-Diacetoxy-3,3-dimethyl-1-oxobutyl)amino]propionic acid (606 cm) was dissolved in 30 m of methylene chloride, and under water cooling, 1-ethyl-3-hydrochloride was dissolved.
(3-dimethylaminopropyl)carbodiimide 422
(2) was added, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off. The residue was then subjected to silica gel column chromatography to obtain 900 ml of the title compound (yield 69%).

Properties; Oil optical rotation [α] o; +17.3 (C=1.0,
CHCj! ! )IR (CIl+-', neat
); νc+0 1754, 166022 1 Mass spectrometry Molecular formula; CsqHsqN30? Theoretical value 6
57.4352 Actual value 657.4357 NMR (δ, CDCj2 3); 0.88 (3H
, t, J=7Hz). 1.02 (3Hs). 1.0
5 (3H, s), 1.19-1.43 (20H, m)
, 1.66-1.77 (21{, m), 1.92-2
．． 09 (4H, m), 2.05 (3H, s), 2.0
8 (3H, s), 2.34 (2H, t, J=7Hz)
, 2.56 (2H, t, J=6Hz), 3.50-
3.71 (2H, m). 3.84 (In, d, J=1
1Hz). 4.02 (IH, d, J=11Hz).
4.89 (IH, s). 5.29-5.42 (2H,
n+), 6.76 (18, t, J=6Hz). 7.1
3 (1 ■, brs). 7.447.52 (4H.m)
．． 7.64 (IH, brs) Example-13 N-[4-(oleoylamino)phenyl]-3-[
N-(2,4-dihydroxy-3,3-dimethyl-1
-oxobutyl)amino]propanamide 2 2 2 ■ N~[4-(oleoylamino)phenyl]3- [N
- (2,4-diacetoxy3,3-dimethyl-1-
657 ml of (oxobutyl)aminocopropanamide was dissolved in 4 d of methanol, and while stirring at room temperature, 1.5 ml of IN aqueous caustic soda solution was further stirred for 30 minutes. After the reaction was completed, 10 ml of water was added and the mixture was extracted with 20% methylene chloride. The methylene chloride layer was washed with water and then with saturated brine, dried over anhydrous sodium sulfate, the solvent was distilled off, and the residue was subjected to silica gel column chromatography to obtain the title compound 49.
5■ (yield 86%) was obtained.

Properties: Melting point 146.2-148. 1°C
Optical rotation [α] D i +10.2' (C=1.
0, CHC423)IR (cm-', nea
t); vt. o 1664 mass spectrometry molecular formula;
C3JsJb O? Theoretical value 573.4141 Actual value 573.4144 NMR (δ, CDCI!.3) i 0.8B(3H
, t, J=7Hz), 0.89(3H,s), 0
．． 95 (3■, s), 1.15-1.43 (20■+
m) 1.62-1.77 (2H, m), 1.92-2
．． 08 (4H, m), 2.34 (28, t, J=7H
z), 2.56 (2H, brs), 3.45 (2}
1, S). 3.58 (2H, brs), 3.96 (
1}1. s). 5.27-5.42 (2H, m). 7
．． 25-7.39(4■+m)+7.48(ILbrs
), 7.71(IN,brs), 8.54(1}1
, brs) Example-14 N-[4-(lauroylamino)phenyl]-3[
N- (2,2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]brobanamide 4-lauroylaminoaniline 250K and 3[N- (
2,2.5.5-tetramethyl-1.3=dioxane-
4-carbonyl) aminocoprobionic acid 223■,
The mixture was dissolved in 30 d of methylene chloride, 181 ml of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride was added under ice-cooling, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off.

The residue was then subjected to silica gel column chromatography to obtain the title compound 381 (yield 72%).

Properties: Melting point: 144.3-144.9°C Optical rotation [α] D: +34.6 (C=1.0.C
HCi! ．． 3) 225 IR (cm-', neat); l/C
．． 0 1664 mass spectrometry molecular formula ic3. H49N3
0S theoretical value 531.3672 Actual value 531.3675 NMR (δ, CDCj2i); 0.88 (3H.t,
J=711z) 0.95(3B,s), 1.04
(3H, s), 1.22-1.40 (16■, m),
1.41 (3H, s), 1.45 (3■, s). 1
．． 68-1.80 (2H, mL 2.34 (2H, t.
J=7FIz), 2.65 (2H, t, J=6Hz)
, 3.27 (IH, d, J=12Hz), 3.50
-3.75 (28, m), 3.68 (IH.d, J=
12Hz), 4.10(IH,s). 7.08 (I
H, d, J=6Hz), 7.16 (IFl.s). 7
．． 46 (2H, d, J=8Hz). 7.49 (2H.
d, J=8Hz). 8.09 (IH, s) Example-15 2-(oleoylamino)phenyl 3-[N-(2.
2,5,5-tetramethyl-1,3-dioxane-4-
carbonyl)amino]propionate 2 2 6 2-oleoylaminophenol 303■ and 3[N-
(2,2.5.5-tetramethyl-1.3=dioxane-4-carbonyl)amino]bropionic acid (259 μ), dicyclohexylcarbodiimide (227 mg), and 4-dimethylaminopyridine (122 μ) were dissolved in 15 m of toluene for 2 hours. The mixture was heated to reflux. After cooling the reaction solution, the crystals formed were removed by filtration, the filtrate was concentrated, and the residue was subjected to silica gel column chromatography to obtain the title compound 445 (yield: 72%).

Properties: Oil optical rotation [α] b i +26.9 (C=1.0,
CBCI! s)IR (Cm-', neat)
;νc+0 1772. 1658 Mass spectrometry Molecular formula; C3aHsaNz O6 Theoretical value 614.4294 Actual value 614.4271 NMR (δ, CDCI!.2); 0.88 (3H
, t, J=71Lz), 0.99(3B,s)+
1.00 (3H.s), 1.22-1.43 (20H.s)
, m), 1.43 (3H, s), 1.47 (31{,
s). 1.65-1.78 (2H, m), 1.93
-2.08 (4H, m) + 2-44 (2H, t, J = 7
Hz) +2.80 (2H, t, J=6Hz), 3.2
8 (LH, d, J = 12Hz), 3.69-3.82 (
2H, n+), 3.68 (LH, d, J=12Hz)
．． 4.09 (1B, s), 5.29-5.39 (2H
, m), 7.00 (IH, t, J=6Hz), 7.0
6-7.12 (2Lm), 7.19-7.27 (10
, m), 8.22 (IH, d, J=8Hz), 8.
39(Ill,s) Example-16 4-(oleoylamino)phenyl 3-[N(2,2
, 5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate p-hydroxyoleoylanilide 565K and 3-[
N-(2.2.5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid 393m
g and dicyclohexylcarbodiimide 345 and 4-
204 mg of dimethylaminopyridine and 15 d of toluene
The mixture was dissolved in water and heated under reflux for 2 hours. After cooling the reaction solution, the resulting crystals were removed by filtration, and the filtrate was concentrated and subjected to silica gel column chromatography to obtain 930 mg (yield: 99%) of the title compound.

Properties: Oily optical rotation [α. ;+18.8 (C=1.0, CH
Cffis)IR (cm-', neat);
vc-o 1760+ 1662229 Mass spectrometry Molecular formula i CzbNseNz Oh theoretical value
614.4294 Actual value 614.4312 NMR (δ, CDCj!s); 0.88 (3H
, t, J=7FIz), 1.00(3H,s),
1.06 (3H, s), 1.23-1.43 (20H
, m), 1.43 (3H, s). 1.45(3H,s
), 1.65-1.78 (2■, m) + 1.93-
2.09 (4H, m). 2.35 (2H, t, J=7H
z), 2.82 (2■, t, J=6Hz), 3.29
(1■1 d, J=12Hz) +3.52-3.7
7 (2H, m), 3.70 (IH, d, J=12Hz
), 4.11 (IH.s). 5.29-5.41 (2
H. m). 6.987.07 (IH.m). 7.0
3 (2H, d.J=8Hz), 7.54 (2H, d.
J=8Hz). 7.18 (IH,s) Example-17 4-(oleoylamino)phenyl 3-[N-(2.
4-Diacetoxy3.3-dimethyl-1oxobutyl)amino]propionate 230 p-oleoylaminophenol 372■ and 3-[N
-(2.4-diacetoxy3.3-dimethyl-1-oxobutyl)aminocopropionic acid (259 µm) was dissolved in 30 methylene chloride, and under water cooling, 1-ethyl hydrochloride was dissolved.
3-(3-dimethylaminopropyl)carbodiimide 2
11■ was added to the mixture, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off. The residue was then subjected to silica gel column chromatography to obtain the title compound 255 (yield: 39%).

Properties: Oily optical rotation [α. ; +19.4 (C=1.Q, C
ICI23) IR (Cm-'+ neat).
; v c+0 1750, 1666 mass spectrometry molecular formula; C3JseNz Os theoretical value 658.419
3 Actual value 658.4191 NMR (δ, CDCf 3); 0.8B (3H,
t, J=7Hz), 1.03 (3H, s). 1.
08 (38, s) + 1.22-1.42 (20H, m
), 1.66-1.78 (2■, m), 1.96-2
．． 07 (4H, m), 2.01 (3H, s), 2.0
4 (3B, s), 2.35 (2H, t, J=7Hz)
．． 2.77-2.82 (2H, m). 3.84 (
LH. d, J=12Hz). 4.05 (IH, d, J
=12Hz), 4.97(IH.s). 5.27-5
．． 42 (2H, m), 6.61 (IH, t, J=6H
z), 7.04 (2B, d, J=8Hz), 7.15
(IH, brs), 7.54 (2H. d. J=8
Hz) Example-18 4-(oleoylamino)phenyl 3-[N(2.4
-dibenzyloxy-3.3-dimethyl=1-oxobutyl)amino]propionate 3- [N- (2.4
-dibenzyloxy-3,3-dimethyl-1-oxobutyl)amino]bropionic acid 200 s, 4-(oleoylamino)phenol 186 s, dicyclohexylcarbodiimide 124 s, and 4-dimethylaminopyridine 6
7) was dissolved in 15 d of toluene and heated under reflux for 2 hours.

After cooling the reaction solution, the formed crystals are filtered, the filtrate is concentrated,
The residue was subjected to silica gel column chromatography,
The title compound 312■ (yield 97%) was obtained.

Properties: Oil optical rotation [α] o i +19.3 (C=1.0,
CHCj! s)IR (ell-', neat)
; ν(+6 1760, 1652233 Mass spectrometry molecular formula; C4, H66N2 06 theoretical value 7
54.4920 Actual value 754.4890 NMR (δ, CDCj! 3); 0.88 (3H
, t. J=7Hz). 0.94 (3H.s), 1
．． 05 (3H, s), 1.20-1.41 (20H,
n+), 1.64-1.75 (2H, m), 1.95
-2.09 (4Fl, m). 2.34 (3H, s),
2.75 (3H, t.J=7Hz), 3.23 (IH
．． t. J=9Hz). 3.61 (2H, dd, J=6
Hz), 3.41 (1■, d, J=9Hz), 3.9
0 (IH, s), 4.34-4.55 (4H, m),
5.29-5.42 (2H, m), 6.95 (2H
, d.J=8Hz), 7.03(IH, d.J=8H
z). 7.23-7.39 (10H.m). 7.5
0(2H, d, J=8Hz) Example-19 4-(oleoylamino)phenyl 3-[N-(2.
4-dihydro3,3-dimethyl-1-oxobutyl)
amino]propionate 23 4 4-(oleoylamino)phenyl 3-[N- (2
,2,5,5-tetramethyl-1,3-dioxane-4
-carbonylamino)probionate 500■ acetic acid 2
The solution was dissolved in a mixed solvent of 0.0d and 10.0d of water, and stirred overnight at room temperature. After the reaction was completed, 20 d of water was added and extracted with methylene chloride. The methylene chloride layer was washed with water and dried over anhydrous sodium sulfate. After distilling off the solvent, the residue was subjected to silica gel column chromatography to obtain the title compound 395■ (yield 85%).
) was obtained.

Properties; Oil optical rotation [α] D; +14.3 (C=1.0,
CHCf! 3) IR (c+n-', neat)
; vc. o 175B, 1662 mass spectrometry molecule 2; C3:lH54N2 0h theoretical value 574.398
1 Actual value 574.3952 NMR (δ, CDC I. 3) i 0.88 (3
Fl, t, J=7Hz), 0.93 (38s),
1.03 (3■, s), 1,214.43 (20H
, m) 1.65-1.71 (2H.m), 1.71-
2.18 (6t{, m), 2.35 (2H, t, J=7
Hz), 2.82 (2H, t, J=6Hz), 3.5
0 (IH, d, J=10Hz), 3.60-3.74
(2H, m) 3.54 (IH d J = 10Hz),
4.04 (IH, s), 5.285.43 (2■, m
), 7.15-7.26 (2H, m), 7.04 (
2H, d, J=8Hz), 7.52(2H, d, J=
8Hz) Example-20 4-(linolenoylamino)phenyl 3-[N- (
2.2,5.5-tetramethyl-1,3-dioxane-
4-carbonyl)amino]probionate 4-linolenoylaminophenol 369■ and 3-[
N-(2.2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]bropionic acid 259■
and dicyclohexylcarbodiimide 227mg and 4-
Dimethylaminopyridine 122■ and toluene 15Id
The mixture was dissolved in water and heated under reflux for 2 hours. After cooling the reaction solution, the crystals formed were removed by filtration, and the filtrate was concentrated and subjected to silica gel column chromatography to obtain the title compound 431■ (yield 7).
1%).

Properties; Oil optical rotation [αL; +20.6 (C=1.0, CHC
L) IR (cm-', neat); vc. o
1760, 1662237 Mass spectrometry Molecular formula; C3bH5Jz Oh theoretical value 6
08.3825 Actual value 608.3836 NMR (δ, CDCj2 3) i 0.9B (3H
, t, J=7Hz). 1.00 (3H, s), 1
．． 06 (3H, s), 1.24-1.42 (88, m
), 1.43 (3H, s), 1.45 (3B, s),
1.64-1.78 (28, m). 2.01-2.1
2 (4H, m), 2.35 (2H, t, J=7Hz)
, 2.72-2.86 (6H, m), 3.29 (18
, d, J=12Hz). 3.52-3.77 (2H, m
), 3.70 (IH, d, J=12Hz), 4.11
(IH, s), 5.28-5.44 (6Fl, m).
7.00 (IH, t, J=6Hz), 7.03 (2
8, d, J=8Hz). 7.15(1[1,s),
7.54 (2H, d, J = 8Hz) Example-21 N-[4-(oleoylthio)phenyl]-3[N
- (2,2,5.5-tetramethyl-1,3dioxane-4-carbonyl)amino]propanamide 2 3 8 S-4-aminophenyl thiooleate 778 ■ and 3
- [N-2.2,5.5-tetramethyl1.3-dioxane-4-carbonyl)amino]propionic acid 518
(1) was dissolved in 301 d of methylene chloride, 422 d of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride was added under water cooling, and the mixture was stirred overnight.

The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off. Next, the residue was subjected to silica gel column chromatography to obtain 1.05 g of the title compound (yield: 83
%) was obtained.

Properties; Oil optical rotation [α]D; +29.8 (C=1.0.CI
CI! ．． a) IR (Cll-', neat)
; J/C-11 1696+ 1666 mass spectrometry molecular formula i C+6H5eNz Os S theoretical value
630.4066 Actual value 630.4069 NMR (δ, CDC l 3) i 0.88 (3H
, t, J=7Hz) ,0.90(3H,s), 1
．． 04 (3H.s), 1.21-1.39 (20H,
m), 1.42 (38, s), 1.46 (3H, s)
, 1.60-1.74 (2Hm). 1.92-2.
09 (4H, m), 2.63 (2H, t.J=7Hz)
．． 2.68 (2H, t, J = 6Hz), 3.28 (I
n, d, J = 12Hz), 3.54-3.75 (2H,
m). 3.68 (II, d, J=12Hz), 4.1
0 (IH, s), 5.30-5.42 (2H, m),
7.08 (IH, t, J=6Hz), 7.35 (2H
．． d, J=8Hz). 7.63 (2H, d, J=8H
z), 8.29 (LH.s) Example-22 N-[4-(oleoylthio)phenyl]-31[
N-(2,4-dihydroxy-3,3-dimethyl-1
-oxobutyl)amino]propanamide N- [4-
(oleoylthio)phenyl]-3[N- (2,2
, 5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanamide 500 μ
d and water 10at! and stirred overnight at room temperature. After the reaction was completed, 20% of water was added and extracted with methylene chloride.

The methylene chloride layer was washed with water and dried with anhydrous sodium sulfate.
After distilling off the solvent, the residue was subjected to silica gel column chromatography to obtain the title compound 406 (yield: 87%).

Properties: Oily optical rotation [α]. H +16.0 (C=1.0, C
HC Il 3) IR (c+n-', neat)
i vc-o 16702 4 1 Mass spectrometry Molecular formula; C3JsaNz Os S theoretical value 590. 3753 Actual value 590.3731 NMR (δ, CDCl3) io. 8B(3H,t,
J=7FIz), 0.91(3H,s), 0.98
(3H, s). 1.20-1.42 (20H, m),
1.65-1.77 (2H, II+), 1.93-2
．． 09 (4Lm), 2.57 (2H, t, J=6Hz)
, 2.66 (2H.t.J=6Hz), 3.25 (2
H, brs), 3.48 (2H, brs), 3.50
-3.69 (2H, m). 4.01(IH,s),
5.30-5.42 (2H, m), 7.28 (2H, d
, J=9Hz). 7.50 (2H.d.J=9Hz)
, 7.54 (2H, d.J=6Hz), 8.62 (I
H. s) Example-23 S-4- (oleoylamino)phenyl 3-[N-
(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanethioate 242 S-4-aminophenyl 3-[N- (2,2.5.
5-Tetramethyl-1,3-dioxane-4carbonyl)amino]propanethioate 281 µ was dissolved in methylene chloride 201 d, followed by pyridine ld under water cooling and stirring, followed by a solution of oleic acid chloride 229 µ dissolved in methylene chloride 3 d. was added dropwise, and the mixture was further stirred for 1 hour. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain the title compound 185 (yield 38%).

Properties: Oil optical rotation [α] o i +7.90 (C=1.0,
CHCf s)IR (cm-'+neat)
; I/c+o 1704, 1652 mass spectrometry molecular formula; C3bH5eNz Os S theoretical value 630.4
066 Actual value 630.4044 NMR (6, CDCj2 3) i 0.8B(3
H, t, J=7Hz), 1.00 (3H, s), 1
．． 05 (3■, s), 1.15-1.42 (20H.
m), 1.42 (3H, s), 1.45 (3H, s)
, 1.65-1.79 (2B, m). 1.92-2.
08 (4H, m) + 2.37 (2H, t, J = 7Hz
). 2.82-3.01 (2■, m), 3.29 (
IH, d, J=12Hz). 3.47-3.69 (2H
, m), 3.69 (IH.d.J=12Hz), 4.
09 (1■.s), 5.29-5.42 (2■.m)
, 6.856.92 (IH.m). 7.16 (LH
, s), 7.34 (2B, d, J=8Hz), 7.
60 (2H, d, J = 8Hz) Example-24 S-4-(oleoylamino)phenyl 3[N- (
2.4-Dihydro3.3-dimethyl1-oxobutyl)amino]propanethioate S-4-(oleoylamino)phenyl 3-[N-(2.2.5.5-tetramethyl-1.3dioxane) -4-Carbonyl)amino]propanethioate 483■ to acetic acid 201+1t! and 10 ml of water, and stirred overnight at room temperature.

After the reaction was completed, 20% of water was added and extracted with methylene chloride.

The methylene chloride layer was washed with water and dried with anhydrous sodium sulfate.
After distilling off the solvent, the residue was subjected to silica gel column chromatography to obtain the title compound 404 (yield: 89%).

Properties: Oil optical rotation [α] n i +8.80 (C=1.0,
CHCi! ．． 3) IR (cm-', neat)
; j/c+0 1691L 16702 45 Mass spectrometry Molecular formula; C*zHsaNz Os S Theoretical value 590.3753 Actual value 590.3762 NMR (δ, CDCj2 3); 0.88 (3H
, t, J=7Hz). 0.91 (3H, a). 1
．． 02 (3H, s), 1.19-1.43 (20H,
m) 1.67-1.79 (2H, m). 1.87-2
．． 17 (6H, m), 2.36 (2H, t.J=7Hz
), 2.92 (2H, t, J = 6Hz), 3.48 (
IH, d, J=12Hz). 3.53 (IH, d, J
=12Hz). 3.56-3.65 (2H, m), 4
．． 01 (IH, s), 5.285.42 (2H, m)
．． 7.12 (IH, t, J = 6Hz), 7.26 (
IH. brs). 7.34 (2H, d, J=8Hz)
, 7.59 (2H, d, J=8Hz) Example-25 S-4-(oleoylamino)phenyl 3-[N-(2.4-diacetoxy3.3-dimethyl-1-oxobutyl)amino] Propanethioate 2 46 Ac-0 Ac-0 S-4-aminophenyl 3-[N-(2.4diacetoxy3.3-dimethyl-1-oxobutyl)amino]propanethioate 276■ in methylene chloride 20d
was dissolved in water-cooled and stirred with 1 pyridine, then 196 ml of oleic acid chloride was added with 3 Il of methylene chloride! i! A solution dissolved in was added dropwise to the mixture, and the mixture was further stirred for 1 hour. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain the title compound 304 (yield 69%).

Properties; Oil optical rotation [α] D i +21.3' (C=1.0
．． CHCj! i) IR (cm-'+ neat
); ν-o 1750, 1670 Mass spectrometry Molecular formula i C+JssNz Oq S theoretical value 674
．． 3964 Actual value 674.3976 NMR (δ, CDCj'+); 0.88 (3H.t
, J=7Hz), 1.00 (3H.s), 1.06
(3■,s). 1.21-1.33 (20H, m),
1.62-1.77 (2H, m). 1.94-2.0
8 (4H.m), 2.06{3Ls). 2.10 (3
}1,s), 2.37 (2Lt.J=7Hz). 2
．． 89 (21, t, J=6Hz). 3.44-3.68
(2H, m). 3.82 (IH, d, J=11Hz)
．． 4.03 (IH, d, J=11Hz), 4.97
(IH.s). 5.29-5.41 (2H, m), 6
．． 47 (IH, t, J=6Hz). 7.19-7.3
2 (2H, m), 7.17 (IH.s). 7.35 (
2H. d, J=8Hz). 7.61 (2H, d,
J=8Hz) Example-26 N-[2-(oleoyloxy)phenyl]-3[N
- (2.2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide N-(2-hydroxyphenyl)-3-[N-(2.2
．． 5.5-Tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide 350■, oleic acid 282mg and dicyclohexylcarbodiimide 227
(2) and 122 mg of 4-dimethylaminopyridine were dissolved in 15 d of toluene and heated under reflux for 2 hours. After cooling the reaction solution, the resulting crystals were removed by filtration, the filtrate was concentrated, and the residue was subjected to silica gel column chromatography to obtain 1 mg of the title compound 41 (yield: 67%).

Properties; Oil optical rotation [α]D; +32.3° (C=1.0, C
ICI 3) IR (cm-', neat);
l/cm0 176B+ 1668249 Mass spectrometry Molecular formula i C3hHssNz O6 theoretical value
614.4294 Actual value 614.4294 NMI? ．． (δ, CDCf 3); 0.88 (3H
, t, J=7Hz), 0.96 (3H, s). 1
．． 03(3H,s), 1.23-1.45(20}1
, m). 1.40 (3H, s). 1.45(3H,s
). 1.71-1.83 (2B, m). 1.92-
2.08 (4H, m), 2.58-2.67 (4H,
m), 3.27 (IH, d, J=12Hz). 3.5
6-3.64 (21, m), 3.67 (IH, d, J=
12Hz). 4.07 (IH.s). 5.305.
42 (2H.m). 7.03-7.17 (3H, m)
．． 7.197.29 (IH, m), 7.49 (IH
, brs), 8.18 (IH, s, J=8Hz) Example-27 N-[4-(oleoyloxy)phenyl]-3[
N-(2,4-diacetoxy3,3-dimethyl-1-
oxobutyl)amino]propanamide 250 N-(4-hydroxyphenyl)-3-[N(2.4-
394 μm of diacetoxy-3,3-dimethyl-1oxobutyl)amino]propanamide was dissolved in 20 m2 of methylene chloride.
1m of pyridine and 301mg of oleic acid chloride were dissolved in 3rd.m of methylene chloride while stirring under water cooling. A solution dissolved in was added dropwise to the mixture, and the mixture was further stirred for 1 hour. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain 530+++ g (yield 81%) of the title compound.
I got it.

Properties; Oil optical rotation [α]n; +14.9° (C = 1. Sail C
HC1s)IR (cm-', neat)
; νc. o 1746+ 1666 mass spectrometry Molecular formula; CsJssNz Oe Theoretical value 658.4193 Actual value 658.4184 NMR (δ, CDCI!.3); 0.88 (38
, t, J=7Hz). 1.02(3Fl,s),
1.05 (38,s), 1.22-1.42 (20H
．． m). 1.68-1.79 (2■, m), 1.94
-2.09 (4Lm), 2.05 (3H, s), 2.
07 (3■, s), 2.51-2.59 (4H, m),
3.54-3.71 (2H, m), 3.84 (IH
, d, J=12Hz). 4.02 (1■.d, J=1
2Hz), 4.88 (IH, s), 5.28-5.4
2 (2H, m), 6.72 (IH, t, J=6Hz)
．． 7.34 (2B, d, J=8Hz). 7.54 (2
H, d, J = 8Hz), 7.71 (IH, brs) Example-28 N-[4-(oleoyloxy)phenyl]-3[N-
(2.4-dihydroxy-3.3-dimethyl-1-oxobutyl)amino]propanamide N-[4-(oleoyloxy)phenyl]3-[
N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanamide 1.
Og was dissolved in a mixed solvent of 20 ml of acetic acid and 10 d of water, and the mixture was stirred at room temperature overnight. After the reaction was completed, 20 d of water was added and extracted with methylene chloride. The methylene chloride layer was washed with water, dried over anhydrous sodium sulfate, the solvent was distilled off, and the residue was subjected to silica gel force column chromatography to obtain the title compound 830.
(1) (yield 89%) was obtained.

Properties; Oil optical rotation Cα] o; +21.0 (C=1.(1
．． CHCI! 3) IR (cm-', neat)
; J/C. 0 1760+ 16602 5 3 Mass spectrometry Molecule 2; C+JsJ20h Theoretical value 574.3981 Actual value 574.3977 NMR (δ, CDCI!.3); 0.8B (3H
, t, J=7Hz), 0.90 (3H, s), 0.
98 (3B, s). 1.19-1.46 (20H.m
), 1.41 (3H, s), 1.68-1.79 (2
1, m), 1.932.09 (4H, m), 2.5
5 (2H, t, J=7Hz), 2.59 (2H, t,
J=6Hz), 2.72 (2H, brs), 3.55
-3.68 (2H, m), 3.48 (2H, s),
3.98 (ILs), 5.295.42 (2H, m)
, 7.45-7.53 (IH, m), 7.00 (2
H, d, J = 8Hz), 7.52 (2H, d, 8Hz
), 8.35(IH,s) Example-29 N-[4-(oleoyloxy)phenyl]-3[
N-(2.2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanamide 25 4 N-(4-hydroxyphenyl kl-[N(2,2,5
．． 5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanamide 1. 44 g of methylene chloride was dissolved in 20 FIr1 of methylene chloride, and while stirring under water cooling, 5 parts of pyridine and then 1 part of oleic acid chloride were added. A solution of 20 g dissolved in 10 d of methylene chloride was added dropwise, and then 1
Stir for hours. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain the title compound 1.
93 g (yield 79%) was obtained.

Properties: Oily optical rotation [α. ; +32.6 (C=1.0,
CHC I! ．． s) IR (cm-', neat
) ; vc. o 1764+ 1668 Mass spectrometry Molecular formula i C3JseNz Oh theoretical value 614.4
294 Actual value 614.4319 NMR (δ, CDCI!.3); 0.88 (3H,
t, J=7Hz)+0.96(3H,s), 1.
04 (3H, s), 1.23-1.45 (20H, m
), 1.41 (3H, s), 1.46 (3H, s),
1.66-1.70 (28, m). 1.93-2.
09 (4H, m) + 2.54 (2H, t, J = 7Hz)
, 2.66 (2■, t, J=6Hz). 3.27 (L
H. d, J=12Hz), 3.52-3.77 (2■,
m), 3.68 (IH, d, J = 12 ■ z) + 4.1
0 (LH, s), 5.29-5.42 (2B, m),
7.017.10 (LH.m), 7.01 (2H,
d, J=8Hz). 7.57 (2H.d, J=8Hz
). 8.11 (IH,s) Example-30 N-[f-(oleoyloxy)phenylco 3[
．． N-(2,4-diacetoxy-3,3-dimethyl-1
-oxobutyl)amino]brobanamide S-p-aminophenyl thiooleate 779 ■ and 3
- [N- (2.4-diacetoxy-3.3-dimethyl-1-oxobutyl)aminocoprobionic acid 606■
was dissolved in 30 yd of methylene chloride, and diluted with hydrochloric acid under water cooling.
442 μl of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide was added, and the mixture was stirred overnight. The reaction solution was washed with water, dried over anhydrous sodium sulfate, and then the solvent was distilled off.

The residue was then subjected to silica gel column chromatography to obtain 780 ml of the title compound (yield 58%).

Properties: oily 25 7 Optical rotation [α] n i +14.5 (C=1.0,
CHCfs)IR (Cll1-'l neat
) ; vc. o 1748, 1672 Mass spectrometry Molecular formula; C+JseNg 07 S theoretical value 674
．． 3964 Actual value 674.3991 NMR (δ, CDCI s); 0.89 (3H,
t, J=7Hz), 1.03 (3■, s), 1.
06 (3H, s), 1.22-1.41 (20H, m
). 1.64-1.75 (2H, m), 1.96-2
．． 08 (4tl, m). 2.05 (38,s). 2.
08 (3H, s), 2.58 (2H, t, J-6Hz
), 2.64 (2H.t, J=7Hz), 3.55
-3.70 (2■, m), 3.85 (IH, d, J=
11Hz), 4.02 (IH, d, J=11H2).
4.87 (IHS). 5.28-5.43 (2H
, m), 6.69 (1■, t, J=6Hz), 7.3
4 (IH, d, J = 8Hz), 7.60 (2H, d, J
=8Hz), 7.81 (1B, brs) Example-31 N-(2-N-oleoylaminoethyl)-3[N-(
2.4-Diacetoxy3,3-dimethyl-1-oxobutyl)amino]propanamide 2 5 8 N-(2-aminoethyl)oleoylamide 1. 0
7 g and 4-nitrophenyl 3-[N- (2.4
-Diacetoxy-3.3-dimethyl-1-oxobutyl)amino]propionate 1. 40 g of the solution was dissolved in 40 m of tetrahydrofuran, and the mixture was stirred at room temperature overnight.

After the reaction was completed, the solvent was distilled off under reduced pressure, the residue was dissolved in ethyl acetate, washed with an aqueous potassium carbonate solution and then with water, the organic layer was dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was subjected to silica gel column chromatography to obtain 4.45 g (yield 75%) of the title compound.

Properties: Oily IR (cm-', neat); vc-o
2980+ 1740+ 1650 mass spectrometry molecular formula; C33H59N3 07 theoretical value・609.435
2 Actual value 609.4342 NMR (δ, CDCj2 3)? 0.88(3
H, t, J=7Hz), 1.05 (3H, s),
1.09 (3H, s), 1.10-1.40 (
18H, m), 1.54-2.42 (12H, m),
2.07 (3H, s), 2.16 (3H, s),
3.20-3.60 (6H, m), 3.86 (
IH, d, J=11Hz), 4.05 (IH, d,
J=11Hz), 4.86(18,s). 5.
30-5.40 (2H, m), 6.14-6.22
(IH, brs). 6.52-6.60 (IH.b
rs). 7.04-7.12elLbrs) Example-32 N-(2-N-oleoylaminoethyl)-3-[N
-(2,4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanamide N- (2-N-
oleoylaminoethyl)-3- [N- (2.4-
diacetoxy (3,3-dimethyl-1-oxobutyl)
200 μm of amino]propanamide was dissolved in 10 m of methanol, and 0.0 μm of 1N caustic soda aqueous solution was added to the mixture while stirring at room temperature.
5 d was added and stirred for 2 hours. After the reaction, the solvent was distilled off under reduced pressure, extracted with ethyl acetate, and the organic layer was washed with water.
It was dried over anhydrous sodium sulfate and the solvent was distilled off. The residue was purified by silica gel column chromatography to obtain 150 ml of the title compound (yield: 86%).

Properties: Oily 26 1 IR (cm-', neat); voH3
324+! 'c-0 1650 mass spectrometry molecular formula i
CzJsJa Os Theoretical value 507.4011 Actual value 507.4044 NMR (δ, CDCfi s) i 0.8B (31
, t, J=711z), 0.94(3H,s). 1
．． 00(3f(,s). 1.16-1.40(17H
, m). 1.50-1.64 (2H.m). 1.92
-2.08 (4H, n+). 2.19 (2H, t, J=
7Hz). 2.30-2.80 (68, m), 3.2
0-3.54(6}1,m), 3.62-3.74(
1}1, m), 4.02 (IH, s). 5.39-5
．． 44 (2H.m), 6.406.50 (IH, sum)
, 6.96-7.04 (IH, m), 7.45-7
．． 53 (IH, m) Example-33 N- (3-N-oleoylaminoprobyl)-3[N
-(2.2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)aminocopropanamide 2 6 2 N-(3-aminopropyl)oleoylamide 3. 3
8 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carponyl)amino]
Probionic acid 2. 5 9 g and aethyl hydrochloride-3
-(3-dimethylaminopropyl)carbodiimide 1.
91 g and 50 Id. of methylene salt. and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The residue was purified by silica gel column chromatography to obtain 4.5 sg (yield: 81%) of the title compound.

Properties: Oily JR (cm-'. neat); νc+(+1
650? Quantitative analysis Molecular formula; C3■HS9N3 0S Theoretical value 565.4455 Actual value 565.4454 NMR (δ, CDCjl! :l) i 0.8B(
3H, t, J=7Hz), 0.97(3H,s),
1.04 (3B, s), 1.23-1.40 (14
H, m), 1.43 (3H, s), 1.47 (H, s
), 1.52-1.86 (6H, s+), 1.92
-2.10 (4N, m), 2.18 (2H.t.J=7
}IZ). 2.46 (2■, t, J=6Hz). 3.
29 (1■, d, J = 12■2) 3.38 (3Lbrs
), 3.44-3.62 (4}1, m), 3.67 (
IH, d, J=12Hz). 4.08 (IH, s).
5.30-5.42 (2 fl, m), 6.20-6
．． 30 (ILbrs), 6.65-6.73 (IH,
brs). 6.99-7.08 (IH, brs) Example-34 N-(3-oleoylaminopropyl)-3[N- (
2.2.5.5-tetramethyl-1,3-dioxane-
4-carbonyl)amino]propanamide N-(3-aminopropyl)oleoylamide3. 3
9 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]
Propionic acid 2. 59 g and 1-ethyl-3 hydrochloride
-(3-dimethylaminopropyl)carpodiimide 1.
91g and 50mi of salted methylene! and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The residue was purified by silica gel column chromatography to obtain 2.7 g (yield: 47%) of the title compound.

Properties: Oily IR (cm-', neat); ! '()6
166026 5 Mass spectrometry Molecular formula i C3sHb+Ns Os theoretical value
579.4611 Actual value 579.4630 NMR (δ, CDCf 3); 0.8B (3B,
t, J=7Hz), 0.97 (3H, s), 1.
04 (3■, s), 1.10-1.40 (20H, n
+). 1.42 (3H, s). 1.46 (3H, s)
, 1.54-1.90 (5H, m), 1.90-2.
10 (3H, m), 2.20 (2Fl.t.J=7Hz
). 2.47 (28, t, J=6Hz). 3.20-
3.36 (5H.m) 3.48-3.66 (2H.m)
．． 3.69 (LH, d, J = 12Hz), 4.08 (
IH, s), 5.30-5.40 (2H, m), 6
．． 15-6.25 (IH, m), 6.58-6.66
(IH, m), ? ．． 027.10 (IH, m) Example-35 N-(3-oleoylaminopropyl)-3[N-(2
．． 4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanamide 26 6 N-(3-oleoylaminopropyl)-3[N-(2
,2,5.5-tetramethyl-1.3dioxane-4-
carponyl) aminocopropanamide 0. 5 8 g
was dissolved in a mixed solvent of 20 d of acetic acid and 10 d of water, and stirred at room temperature overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain 0.48 g (yield: 89%) of the title compound.

Properties: Oily IR (cl', neat) i vc-o 16
50 mass spectrometry molecular formula ic3. HS? N! OS theoretical value 539.4297 Actual value 539.4291 NMR (δ, CDC I J i 0.88 (3H,
t, J=7Hz) ,0.90(3H,s),
1.01 (3H, s), 1.20-1.40 (20
H, m) 1.55-1.68 (4H, m), 1.9
2-2.08 (4H, 1M), 2.19 (2■, t, J
=6Hz). 2.36-2.54 (2Lm), 3.
16-3.40 (6H, m), 3.48 (2H, s
), 3.423.56 (ILm). 3.62-3
．． 76 (LH, m), 4.00 (IH, s), 5
．． 28-5.42 (2H, m), 6.18-6.24
(ILmL6.85-6.94 (IH, m), 7.4
2-7.52 (IH, m) Example-36 N-(3-oleoylaminopropyl)-3[N-(2
．． 4-Diacetoxy-3.3-dimethyl-1-oxobutyl)amino]propanamide [N-(2.4-dihydroxy-3.3-dimethyl-1-oxobutyl)amino]propanamide 0. 54 g was dissolved in pyridine 5-, 101I1 of acetic anhydride was added, and the mixture was stirred overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain 0.62 g (yield: 99%) of the title compound.

Properties: Oily IR (CI!1-', neat); ! Ic-
0 173EL 1658 Mass spectrometry Molecular formula; C, 4■
brNs Oq Theoretical value 623.4508 Actual value 623.4499 NMR (δ, CDCfs); 0.88 (3H.t
, J=7■Z). 1.04(3H,sL 1.08(
3H. s). 1.16-1.50 (23H.m). 1
．． 56-1.72 (21, m), 1.90-2.06
(2H, m), 2.07 (3H.s), 2.15 (3
H,s). 2.19 (2■, t, J=7HZ), 2
．． 46 (2H, t, J=6Hz), 2.32-2.4
8 (2H, m). 3.16-3.40 (5H.m),
3.48-3.62 (2H, m), 3.86 (IH.
d. J=11Hz). 4.03 (IH.s). 4
．． 90 (IH, s), 5.28-5.40 (2H, m
). 5.95-6.0626 9 (IH, m), 6.60-6.70 (1■, m),
7.18-7.28 (IH. m) Example-37 N-(4-oleoylaminobutyl)-3[N- (2
,2,5.5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propanamide N-(4-aminobutyl)oleoylamide3. 7
7 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid2. 59 g and 1-ethyl-3-hydrochloric acid
(3-dimethylaminopropyl)carbodiimide 1.9
1 g was dissolved in 50 m of methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The residue was purified by silica gel column chromatography to obtain 2.66 g (yield: 45%) of the title compound.

Properties: Oily IR (cin-', neat); ν-o 16
4B mass spectrometry molecular formula; C34■63N3 osNMR
(δ, Example theoretical value 593.4768 Actual value 593.4797 CDCj2 s); 0.88 (3H, t, J=7
Hz), 0.97 (31,s). 1.04 (3
H,s). 1.20-1.40 (18H, m). 1
．． 43 (38, s). 1.46 (3H, s).
1.50-1.70 (6H, m). 1.86-2.
10 (6El, m). 2.16 (20, t, J=8■z
L2.45 (2H, t, J=6Hz), 3.20-
3.32 (51, m), 3.42-3.66 (2H, m
), 3.69 (IH, d, J=12Hz). 4.0
8 (IH.s). 5.26-5.42 (2H, +n
), 5.785.86 (IH, m), 6.35
-6.45 (IH, m), 7.027.12 (IH
, m) 38 (4-oleoylaminobutyl i3-[N(2,4-dihydroxy-3.3-dimethyl 1-oxobutyl)amino]propanamide N N-
(2,2.5.5-tetramethyl-1.3dioxane-4-carbonyl)amino]propanamide 1. 1
Dissolve 9 g in a mixed solvent of 20 acetic acid and 10 m of water,
Stir overnight at room temperature. After the reaction is complete, the solvent is distilled off under reduced pressure.
The residue was purified by silica gel column chromatography to obtain 0.43 g (yield: 39%) of the title compound.

Properties: Oily IR (cm-', neat); vc. o 1
650 mass spectrometry molecular formula; CsrHsrN. Os theoretical value 553.4455 Actual value 553.4474 NMR (δ, CDCf 3) i 0.8B (3H.
t, J=711z) IO. 95 (3FI.s), 0
．． 99 (3H, s), 1.18-1.40 (17H,
m), 1.40-1.66 (6B, m), 1.92-
2.10 (4H.m). 2.18 (2H, t, J=6H
z), 2.40-2.50 (28, n), 2.70-
3.32 (6■, m), 3.32-3.72 (6H,
m). 4.00(IN,s). 5.30-5.42 (
2}1. m). 6.04-6.10 (LH, n+),
6.60-6.70 (1B, m), 7.42-7.
52 (IH, w+) Example-39 N-4-(oleoylaminobutyl) -3- [N-
(2.4-diacetoxy3.3-dimethyl1-oxobutyl)amino]propanamide 273 N-(4-(oleoylaminobutyl)-3[N-(2
．． 4-dihydroxy-3.3-dimethyl-1-oxobutyl)amino]propanamide 0. 55 g was dissolved in pyridine 5d, 10 m2 of acetic anhydride was added, and the mixture was stirred overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain the title compound 0.
．． 52 g (yield 82%) was obtained.

Properties: Oily IR (cm-'+ neat); νc++1
1730+ 1650 mass spectrometry Molecular formula; G3sNb
3Nz 07NMR (δ, theoretical value 637.4566 actual value 637.4584 cock 3); 0.88 (3■, t, J=7Hz
), 1.03 (3H, s), 1.07 (3H,
s), 1.20-1.40 (18H, m), 1.5
04.70 (6■.m), 1.70-2.10 (6
}1, m), 2.07 (3H, s), 2.16 (3
Ls), 2.16 (2H, t, J=7Hz),
2.38 (2H, t, J=6Hz). 3.20-3.3
0 (4H, m), 3.42-3.62 (2H, n+
), 3.85 (IH, d, J=11Hz), 4
．． 20 (1■, d, J = 11Hz), 4.93 (I
H, s), 27 4 5.30-5.42 (2H, m), 5.76-5.8
6 (1B, m), 6.22-6.30 (LH, m).
7.00-7.08 (1■+m) Example-40 N- (5-oleoylaminobentyl)-3[N-
(2,2.5.5-tetramethyl-1.3dioxane-
4-carbonyl)amino]brovanamide N-(5-aminopentyl)oleoylamide 3.6
6g and i [N- (2,2,5.5-tetramethyl-
1.3-dioxane-4-carbonyl)amino]probionic acid2. 59 g and 1-ethyl-3-(3
-dimethylaminopropyl)carbodiimide 1.91g
was dissolved in 50% methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The residue was purified by silica gel column chromatography to obtain 3.64 g (yield: 60%) of the title compound.

Properties: Oily IR (c+++-', neat); ν(+6
1660 mass spectrometry molecular formula; CisH6sTo O
sTheoretical value 607.4923 Actual value 607.4906 CDCffis) io. 8B (3H.t, J=7Hz
). 0.97(3H.sL 1.04(3H,s),
1.20-1.74 (30H, m), 1.46 (3H
, s), 1.48 (3H.s), 1.90-2.10
(4H, m) + 2.16 (2H, t, J=7Hz).
2.44 (2■, t, J=7H2), 3.24 (2
H, dt, J=6Hz, 7Hz), 3.29(LH,
d, J=12Hz), 3.44-3.66 (2H, m
), 3.68 (IH, d, J=12Hz), 4.0
7 (IH.s), 5.32-5.44 (2H, m),
5.54-5.62 (IH, m), 6.05-6.
12 (IH, m), 6.96-7.08 (LH, m)
Example 41 NMR (δ, N-(6-oleoylaminohexyl)-3[N-(
2,2.5.5-tetramethyl-1.3=dioxane-
4-carbonyl)amino]propanamide N-(6-aminohexyl)oleoylamide 3.81
g and 3-[N- (2,2,5.5-tetramethyl-1
．． 3-Dioxane-4-carbonyl)amino]propionic acid2. 59 g and 1-ethyl-3-(3-
1.91 g of dimethylaminopropyl) carbodiimide was dissolved in 50 m of methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried with anhydrous sodium sulfate,
The solvent was distilled off.

The residue was subjected to silica gel column chromatography.
7 and purified to obtain 2.92 g (yield 47%) of the title compound.

Properties: Oily IR (cm-'+ neat); pc-o 1
664+ 1644 mass spectrometry molecular formula; C36H67
N! OS theoretical value 621.5080 Actual value 621.5057 NMR (δ, CDC I!.3); 0.8B(3
H, t, J=7Hz), 0.97 (3H, s).
1.04 (3H, s), 1.18-1.76 (32
[1, m) 1.42 (38, s), 1.46 (3H,
s), 1.92-2.10 (4H, m), 2.15 (
2H. t. J=7Hz), 2.44(2H,t,J=
7Hz). 3.23 (2H.dt, J=6Hz, 7H
z). 3.29 (IH, d, J=12Hz). 2.
44-3.66 (4H, m). 3.68 (IH, d,
J=12Hz). 4.07 (IH, s), 5.30
-5.42 (2H, m), 5.48-5.58 (IH
, m). 5.96-6.06 (IH, m), 7.0
0-7.06 (IH.m) Example 42 N- (8-oleoylaminooctyl)-3[N-
(2,2,5.5-tetramethyl-1.3dioxane-
4-Carbonyl)amino]propanamide N-(8-aminooctyl)oleoylamide4.
08 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]probionic acid2. 59 g and 1-ethyl hydrochloride
3-(3-dimethylaminopropyl)carbodiimide 1
．． 91 g was dissolved in 50 d of methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The residue was purified by silica gel column chromatography to obtain 1.36 g (yield 21%) of the title compound.

Properties: Oily IR (cm-', neat); νctQ
1664+ 1644 mass spectrometry molecular formula; Cie
H7+Ns Os theoretical value 649.5392 Actual value 649.53886 NMR (δ, CDCj!3); 0.88 (3H, t
, J=7Hz), 0.97(38,s). 1.04
(3H.s). 1.20-1.40 (27H, m),
1.42 (3H, s), 1.46 (3■, s), 1.
56-1.72 (4H.m), 1.92-2.10 (
4H, m). 2.15 (2H, t, J-7Hz),
2.43 (2H, t, J=7Hz), 3.18-3.
26 (5H, m), 3.28 (IH.d.J=12H
z), 3.44-3.66 (48, m), 3.68
(IH, d, J=12Hz), 4.07 (IH, s)
．． 5.30-5.40 (2H, m). 5.40-5.
48 (1■, m), 5.865.94 (IH, m),
6.98-7.06 (IH, m) Example 43 N-(2-oleoyloxyethyl)-3-[N- (
2,2,5.5-tetramethyl-1,3-dioxane-
4-Carbonyl)amino]propanamide 2-aminoethyl oleinate3. 2 6 g and 3
- [N- (2,2.5.5-tetramethyl-1.3
-dioxane-4-carbonyl)amino]propionic acid2. 59 g and 1.91 g of 1-ethyl-3-(3-dimethylaminopropyl)carpodiimide hydrochloride were dissolved in 50 m of methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography to obtain 1.75 g of the title compound (yield 31%).
) was obtained.

Properties: Oily IR (Cll1-', neat); νe-6
1742. 1660 mass spectrometry molecular formula H C:+Js
sNz Oh theoretical value 566.4294 28 1 Actual value 566.4304 NMR (δ, CDC13); 0.88 (3H,
t, J=7Hz), 0.97 (3H, s). 1.04
(3Fl,s). 1.16-1.40 (H+m)
+1.42 (3H.s), 1.46 (3H.s). 1
．． 52-1.70 (4H, m), 1.70-1-90
(2H, m), 1.96-2.08 (2Lm) + 2.3
2 (2H.t.J=7■z). 2.46 (2■, L
J=7Hz) l3.29(IH, d, J=12Hz
). 3.42-3.66 (4H, m), 3.68 (I
H. d. J=12Hz), 4.07(1■.S). 4
．． 15 (2H, t, J=12Hz), 5.32-5.
40 (21+, m). 6.08-6.18 (IH, m)
．． 6.98-7.08 (IH, m) Example 44 2-N-oleoylaminoethyl-3-[N(2.2,
5.5-Tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 282? -(2-hydroxyethyl)oleoylamide 0.
9 7 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]
Bropionic acid 0. 78 g, 0.61 g of dicyclohexylcarbodiimide and 0.61 g of 4-(N,N-dimethylamino)pyridine. 36 g was dissolved in 30 parts of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 1.50 g (yield: 90%) of the title compound.

Properties: Oily IR (cm-', neat); vc-of
742+ 1658 mass spectrometry molecular formula ic3■HseN
z 06 Theoretical value 566.4254 Actual value 566.4274 NMR (δ, CDC l a); 0.88 (3H
, t, J=7Hz), 0.98(38,s),
1.03 (3H, s), 1.22-1.38 (18H
, m), 1.43 (3Ls). 1.47(3H,s>
．． 1.50-1.72C5H, m), 1.92-2
．． 08 (4H, m), 2.21 (2H, t, J=7
H2), 2.56 (2H, t, J=6Hz),
3.29 (LH, d, J=12Hz), 3.42-
3.70 (4tl, m), 3.66 (IH, d, J
=12Hz). 4.08 (IH, s), 4.1
8 (LH, s), 5.285.40 (2H, m),
6.27-6.38 (LH, brs), 6,8
86.96 (IH, brs) Example 45 2-(N-oleoylamino)ethyl-3-[N(2.
4-dihydroxy-3,3-dimethyl 1-oxobutyl)amino]propionate 2-N-oleoylaminoethyl 3-[N(2,2,5.5-tetramethyl-1,
880 mg of 3-dioxane-4-carbonyl)amino]propione was dissolved in a mixed solvent of 20 d of acetic acid and 10 d of water, and stirred overnight at room temperature. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain the title compound 740■ (yield 91%).
I got it.

Properties: Oily IR (cm-', neat); ! /811
3324+ pc-o 1740+ 1650 mass spectrometry molecular formula; CzJsJz Oh theoretical value 526. 3
952 Actual value 526.3961 NMR (δ, CDCj! !!) i 0.8B (3H
, t, J=7Hz), 0.94 (3H.s), 1
．． 04 (3H, s). 1.20-1.40 (20H,
m), 1.52-1.68 (2H, m), 1.90-
2.10 (3■, m), 2.20 (2H, t, J=7F
Iz), 2.49-2.58 (2■+m)+2.80
-3.30 (3■, m), 3.38-3.76 (6H
, n+), 4.02 (II, s), 4.05-5.4
2(2■+m)+6.20-6.30(1}1, b
rs), 7.30-7.40 (IH, brs) Example-46 2-(N-methyl-N-oleoylamino)ethyl 3
- [N-2.2,5.5-tetramethyl2 8 5 1.3-dioxane-4-carponyl)amino]propionate N-methyl-N-(2-hydroxyethyl)oleoylamide 3. 40 g and l- [N- (2,2.5
,5-tetramethyl-1,3-dioxane-4carbonyl)amino]brobionic acid2. 59 g and dicyclohexylcarpodiimide2. 0 6 g and 41 (N
, N-dimethylamino)pyridine1. 2 2g and 30m of toluene! The mixture was dissolved in water and heated under reflux overnight.

After the reaction was completed, it was cooled, the precipitate was removed, and the organic layer was diluted with 1N hydrochloric acid,
It was washed with water and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by column chromatography on 286 silica gel to obtain 3.42 g (yield: 59%) of the title compound.

Properties: Oily IR (cm-', neat) iv. ．． o 1
740, 1658 Mass spectrometry Molecular formula i C33H60
NZ 06 Theoretical value 580.4452 Actual value 580.4478 NMR (δ, CDC I!.3) i 0.88 (3
■, t, J=7Hz), 0.97 (3■, s),
1.04 (38,s), 1.22-1.42 (19H
．． m), 1.43 (3■, s), 1.47 (3H, s
), 1.55-1.70 (3H, m). 1.90-
2.10 (4H, m). 2.30 (28,tt,J=
7B2.7HZ), 2.52-2.60 (2H, II
1), 3.05 (38, s), 3.29 (18, d
, J=12Hz). 3.42-3.67 (4H, m)
, 3.68 (IH, d, J=12Hz), 4.08
(IH, s), 4.24 (2H, t, J=7Hz).
5.30-5.42 (2B, m) 6.98-7.08 (
1■tno) Example-47 3-N-oleoylaminopropyl 3-[N-(2,
2,5,5-tetramethyl-1,3-dioxane-4-
carbonyl)amino]probione N-(3-hydroxyprobione)oleoylamide3. 40 g and 3-
[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carponyl)amino]probionic acid2.
5 9 g and dicyclohexyllupodiimide 2.
0 6 g and l-(N,N-dimethylamino)pyridine 1. 22 g was dissolved in 30 Id of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 4.52 g (yield: 78%) of the title compound.

Properties: Oily IR (cm"', neat); vc-
o 174 (L 1654 mass spectrometry molecular formula i C3
J6oNz O6 theoretical value 580.4450 Actual value 580.4449 NMR (δ, CDCj! 3) i 0.88 (3H
．． t, J=7Hz), 0.98(3H,s),
1.04 (3H, s). 1.10-1.50 (21H
, m), 1.43 (3H, s). 1.46(3H,s
), 1.52-1.86 (2H, m), 1.84 (
21,tt,J=6tlz,7Hz), 1.90-2
．． 10 (3H, m), 2.17 (2■, t, J=7H
z). 2.56 (2H, t, J=6Hz), 3.2
8 (1■, d, J=12Hz). 3.33(2■,d
d, J=6Hz. 7Hz), 3.35-3.60(2
H, II1), 3.68 (LH, d, J = 12 ■ z)
+ 4.08 (IO.s), 4.15 (2FI, t.
J=7Hz), 5.28-5.42 (2H.m).
5.92-60.2 (18,brs). 6.90-7
．． 00 (IH, brs) Example-48 3-(N-oleoylamino)propyl 3-[N-(
2.4-dihydroxy-3.3-dimethyl-oxobutyl)aminocopropionate 28 9 3-N-oleoylaminopropyl 3-[N(2.2
, 5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionate 0. 58 g was dissolved in a mixed solvent of 20 N1 acetic acid and 10 N1 water, and the mixture was stirred at room temperature overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain 0.49 g (yield: 90%) of the title compound.

Properties: Oily IR (cm-', neat"); J/c+a
1740, 1652 mass spectrometry molecular formula ics. H5
bNz Oa Theoretical value 540.4145 Actual value 540.4138 290 NMR (δ, CDCl3); 0.8B(3
H, t, J=7Hz), 0.93(3■,s)
．． 1.04 (3H.s). 1.18-1.40
(19H.m), 1.52-1.66 (2H,m),
1.83 (2H, tt, J=6Hz, 7Hz),
1.92-2.06 (4H, m), 2.19 (2H
, t, J=6Hz). 2.46-2.72 (2H,
m), 3.00-3.56 (OH, m). 3.
64-3.76 (IO, m), 3.98-4.10
(IH, m). 4.03(LH,s), 4.19-
4.30 (11, m). 5.28-5.42 (2H
, m), 5.86-5.98 (IH, m). 7
．． 44-7.52 (IH, m) Example-49 3-(N-oleoylamino)propyl 3-[N-(
2.4-Diacetoxy 3.3-dimethyl-1-oxobutyl)amino]propionate 3-(N-oleoylamino)propyl 3-[N-(2.4-dihydroxy-3.3-dimethyl-1-oxobutyl) 540 ml of amino]propionate was dissolved in 5 id of pyridine, 10 parts of acetic anhydride was added, and the mixture was stirred overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain 500 mg (yield: 80%) of the title compound.

Properties: Oily IR (cm-', neat); νc-o 17
40, 1650 Mass Spectrometry Molecular Formula i C34H6. N
Z OIl Theoretical value 624.4348 Actual value 624.4323 NMR (δ, CD(J!3); 0.88 (3FI,
t, J=7Hz), 1.04 (3H, s), 1.0
7 (3H, s), 1.15-1.40 (21■+In
)+1.55-1.72 (2H, m). 1.84'(
2H. tt, J=6Hz, 6Hz), 1.92-2.
10 (3■, m), 2.07 (3H, s), 2.15
(3■, s), 2.16 (2H, t, J=7Hz),
2.54 (2H.t, J=6Hz), 3.20-3
．． 68 (41, m), 3.83 (IN, d, J=11
}1z), 4.09 (ILd, J=IIHz), 4.
12 (2H.d, J=6Hz). 4.93 (IH,
s), 5.305.38 (2H.m), 5.9
2-6.02 (IH, +w). 6.706.80(
18,m) Example-50 3-(N-oleoylamino)propyl 3-[N-
(2,4-dibenzyloxy-3,3-dimethyl-1-
oxobutyl)amino]propionate 3-(N-oleoylamino)propyl 3-[N-
(2,4-dihydroxy-3.3-dimethyl-1-oxobutyl)amino]propionate (270 µ) was dissolved in pyridine 5jd, and 281 µ of benzoyl chloride was added thereto and stirred overnight. After the reaction, the solvent 293 was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain the title compound 260 (yield: 69%).
) was obtained.

Properties: Oily IR (cm-', neat); vc. o 1
722, 1650 mass spectrometry Molecular formula: CaaHba
Nz Os theoretical value 748.4662 Actual value 748.4673 NMR (δ, CDC7!3); 0.88 (3L
t, J=7Hz), 1.20-1.40 (25H, m)
, 1.52-1.64 (2■, m), 1.76 (2
H, tt, J=6Hz, 7Hz). 1.92-
2.06 (48, m). 2.11 (2H.t, J=7H
z), 2.51 (2H, t, J=6Hz), 3.18
-3.40 (2H, m), 3.40-3.66 (2H
, m). 4.02 (2H.t, J=6Hz). 4.2
8 (IH, d.J=10Hz), 4.33 (1■.d,
J=10Hz), 5.30-5.40 (2H, m),
5.82-5.92 (IH.m), 6.78-6.8
6 (1■, II1). 7.40-7.50 (4H.m)
, 7.52-7.64 (2fl.m). 8.00-8
．． 10(4H,m) Example-51 3-(N-oleoylamino)probyl 3-294 [N-C4-penzyloxy-2-hydroxy-3.3
-dimethyl-1-oxobutyl)amino]probionate 3-(N-oleoylamino)propyl 3[N-(2
．． 4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]probionate 540
The mixture was dissolved in Idl, 140 μm of benzoyl chloride was added, and the mixture was stirred overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain the title compound 318 (yield: 51%).

Properties: Oily IR (cm-', neat); vc-o 1
740. 1720+ 1660 Mass Spectrometry Molecular Formula i.
csJ6oNz O6 theoretical value 628.4449 Actual value 628.4423 NMR (δ, CDCffi 3); 0.8B(3
H, t, J=7Hz), 1.06 (3H, s),
1.18 (3H.s), 1.16-1.40 (17H.s)
．． n+), 1.48-1.62 (28, m). 1.6
2-1.70 (3H.m) 1.81 (2H, tt, J=
7Hz, 7Hz). 1.92-2.08 (3H, m)
．． 2.11 (3H.t, J=7Hz). 2.42-
2.70 (2H, m). 3.18-3.30 (IH,
m), 3.34-3.48 (2H, m). 3.64-3
．． 76 (In.m), 4.00-4.05 (2H, m
), 4.12 (IH, d, J=12Hz), 4.14
-4.24 (IH, m), 4.38 (IH.d, J=1
2Hz) ,4.64-4.68(1■+brs)+5
．． 28-5.40 (2H, m). 5.72-5.82
(IF!.brs). 7.30-7.38 (IH, m)
, 7.44 (2H, dd, J=7Hz, 7Hz),
7.56 (IH, dd, J=7Hz, 7Hz), 8.
05 (2H, d, J = 7Hz) Example-52 3-N-oleoylaminopropyl 3-[N-(2-
Phenyl-5,5-dimethyl-1,3-dioxane-4
-carbonyl)amino]probionetoph N- (3-hydroxyprobione)oleoylamide Fa
40g and 3IN(2-phenyl-5
．． 5-dimethyl-4-carbonyl)amino]probiotic acid3. 0 7 g and dicyclohexylcarbodiimide 2
．． 0 6 g and 4-(N,N-dimethylamino)pyridine 1. 22 g was dissolved in 301d of toluene and heated under reflux overnight. After the reaction is complete, cool and remove the precipitate.
The organic layer was washed with 1N hydrochloric acid, water and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography.
5.34 g (yield: 829.75%) of the title compound was obtained.

Properties: Oily IR (cm-', neat); νc+o 1
738. 1662 mass spectrometry molecular formula; CsJ6oN
z Oh theoretical value 628.4452 Actual value 628.4465 NMR (δ, CDCf3) io. 8B (3H.t,
J=7Hz). 1.11(3H,s), 1.20(
3H, s), 1.22-1.43 (13H, m), 1
．． 52-1.72 (6H, m), 1.77 (2H,
tt, J=7Hz, 7Hz), 1.90-2.06(
4H, m). 2.14 (2■, tt, J=7Hz, 7
Hz). 2.38 (2H, t, J=7Hz), 2.
52 (2H, t, J=7Hz). 3.26 (IH, d
t, J=6tlz, 7Hz). 3.46-3.62 (4
H, m), 3.69 (IH.d, J=12Hz), 4
．． 10 (IH, t, J=7Hz), 4.11 (IH,
s). 5.305.42 (28, m). 5.52 (
In, s), 5.82-5.92 (IH, m). 6.
90-7.04 (IH, m). 7.38-7.44 (3
H, River), 7.48-7.53 (2) l. Il1) Example-53 3-N-oleoylaminoprobil 3-[N-(3,
3-dimethyl-1.5-dioxaspiro29 8 [5.5] nate 3 carbonyl) amino] propio N-(3-hydroxybrobyl) oleoylamide 3.
40 g and 3-[N- (3.3-dimethyl 1,
5-dioxaspiro[5.5]-3-carponyl)amino]probionic acid2. 9 9 g and dicyclohexylcarpodiimide2. 0 6 g and 4-(N,N-dimethylamino)pyridine 1. 22 g was dissolved in 301Ii of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 5.46 g of the title compound (yield: 88
%) was obtained.

Properties: Oily IR (cm-', neat); vc-o 1
740, 1652 mass spectrometry molecular formula i CzbHba
Nz Oh theoretical value 620.4763 Actual value 620.4761 NMR (δ, CDC I!.3); 0.8B(3
H, t, J=7Hz), 0.98(3H,s),
1.03 (3H, s), 1.22-2.10 (36
H, m), 2.17 (2H, t, J=7Hz), 2.
56 (2H, t, J=6Hz). 3.26 (IH, d,
J=12Hz), 3.32(2H, dt, J=6Hz
,7Hz), 3.50-3.68(4B,n+),
3.71 (1B, d, J = 12Hz), 4.10 (I
H, s), 4.15 (2H, t, J=7Hz), 5.
28-5.40 (2H, m), 5.90-5.98 (
1■,m), 6.98-7.10 (LH.m) Example-54 3-(N-oleoylamino)probyl 3[N-(2
-Hydroxy-3,3-dimethyl-4(trimethylacetyl)oxy-1-oxobutyl)amino]propionate 3-(N-oleoylamino)probyl 3[N- (
2,4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propionate (540) was dissolved in pyridine (540)
The mixture was dissolved in Id, 220 μm of pivaloyl chloride was added, and the mixture was stirred overnight. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain the title compound 139 (yield: 22%).

Properties: Oily IR (cm-'. neat); νc. o 1
740+ 1660NMR (δ, CDCfi); 0
．． 8B (3H, t, J=7Hz), 1,201.38
(25H, m). 1.59 (9H, s). 1,52
4.7030 1 (2H, n+), 1.85 (2H, tt, J=7H
z, 7Flz), 1.942.06 (6H, m),
2.17 (2H, t, J=7Hz). 2.56
(2H, t, J=7Hz). 3.28-3.40 (2
H, m), 3.543.62 (2H, +n), 4.
07 (1B, d.J=12Hz). 4.104.20
(2H, m). 4.68 (IH, d, J=12Hz)
．． 5.11 (IH, s), 5.28-5.40 (2
Fl, m). 5.70-5.80 (IH, m),
6.94-7.02 (IH, m) Example-55 3-N-hexanoylaminoprovir 3-[N(2,
2,5,5-tetramethyl-1,3-dioxane-4-
carbonyl)amino]propionate N-(3 hydroxybropyl) hexanoyl 302 amide 1.75 g and 3-[11- (2,2,5,5
tetramethyl-1,3-dioxane-4-carponyl)
Amino]probionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 4-(N,N
-dimethylamino)pyridine1. 22 g of the solution was dissolved in 30 ml of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 1.90 g of the title compound (yield: 46
%) was obtained.

Properties: oily IR (am-'+ neat); vc-o 1
740+ 1658 mass spectrometry molecular formula; C21H38
NZ 06 Theoretical value 414.2730 Actual value 414.2741 NMR (δ, CD(,I!.3); 0.90(3
H. t, J=7Hz), 0.98(3H,s),
1.04 (3■, s), 1.22-1.36 (38,
m), 1.43 (3H, s), 1.46 (3H, s)
, 1.58-1.74 (IH, m), 1.85 (2■
, tt, J=7Hz, 7Hz). 2.18(21,t
, J=7Hz), 2.56(2H,t,J=7Hz
), 3.29 (LH.d, J=12Hz). 3
．． 33 (2H, dt, J=6Hz, 7Hz), 3.
463.66 (4H, m), 3.68 (IH, d,
J=12Hz). 4.08 (IH.s), 4.
16 (2H, t, J=12Hz). 5.94-6.
02 (11, m), 6.92-7.04 (LH, +
n) Example-56 3-N-hexanoylaminopropyl 3-[N(2,
2,5,5-tetramethyl-1,3-dioxane-4-
carponyl)amino]propionate N-(3-hydroxybropyl)octanoylamide2. 03 g and 3-[N-(2,2,5,5tetramethyl-1,3-dioxane-4-carboxyl)amino]propionic acid2. 5 6 g and dicyclohexylcarbodiimide 2. 0 6 g and 4-(N,N-
dimethylamino)pyridine 1. 22 g was dissolved in 30 d of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 2.91 g of the title compound (yield: 66%).
) was obtained.

Properties: Oily IR (cm-', neat); l'e+0
1738+ 1658 mass spectrometry molecular formula; C! 3H4
■N206 theoretical value 442. 3043 Actual value 442.3054 NMR (δ, CDCj2 3): 0.88 (3H
, t, J=7Hz), 0.98 (3■, s). 1
．． 04 (3H, s), 1.20-1.36 (5■, I
II). 1.42 (3H, s). 1.46(3H,s
), 1.56-1.74 (3H, m). 1.84 (2
H,tt,J=7Hz. 7Hz). 2.17 (2■,
t, J=7Hz), 2.56(2H.t, J=7Hz)
). 3.29 (IH, d, J=12HZ). 3.3
3 (2H, dt, J=6Hz, 7Hz), 3.463
0 5 3.66 (4■, m), 3.68 (IH, d, J=1
2■Z). 4.08 (IH.s). 4.15 (2H
．． t, J=7Hz), 5.94-6.02 (IH, river). 6.92-7.04 (LH.m) Example-57 3-N-decanoylaminopropyl 3-[N-(2,
2.5.5-tetramethyl-1,3-dioxane-4-
carponyl)amino]probionate N-(3-hydroxypropyl)decylamide 2,29
g and 3- [N- (2,2,5.5-tetramethyl-
1,3-dioxane-4-carbonyl)amino]propionic acid2. 5 9 g dicyclohexylcarbodiimide 2. 0 6 g and 4-(N,N-dime306 thylamino)pyridine 1. 2 2 g and 3 toluene
The mixture was dissolved at 0 d and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 4.61 g (yield: 98%) of the title compound.

Properties: Oily IR (cm-', neat); ! 'e+0
174 (L 1662 mass spectrometry molecular formula; CzsFl
4Jh 0&Theoretical value 470.3356 Actual value 470.3377 NMR (δ, CDCf 3); 0.88 (3H,
t, J=7Hz). 0.98 (3■s). 1.0
4 (3H, s), 1.20-1.34 (6■, m),
1.42 (3H, s). 1.46 (3H, s), 1
．． 56-1.78 (4H, m), 1.82-1.94 (
3H. m), 2.17 (28, t, J = 7Hz),
2.36-2.44 (LH, n+), 2.56 (2H
, t, J=7Hz), 3.29(10, d, J=12H
z), 3.33 (2■, dt, J=6■z, 7Hz)
, 3.46-3.66 (4H, m). 3.68 (I
H, d, J = 12Hz). 4.08 (1■.s)
．． 4. 15 (2H, t, J=12Hz),
5.92-6.02 (IH, m), 6.08-6.
18 (IH, m), 6.92-7.07 (IH, m) Example-58 3-N-dodecanoylaminoprovir 3-[N(2,
2,5,5-tetramethyl-1,3-dioxane-4-
carbonyl)amino]probionate N-(3-hydroxypropyl)dodecylamide2.
57 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 4-(N,N-dimethylamino)pyridine 1. 22g of the solution was dissolved in 30ml of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 3.19 g (yield: 64%) of the title compound.
I got it.

Properties: Oily IR (cm-', neat); vc. o 1
73B+ 1660 mass spectrometry molecular formula iczJs. N2
0, Theoretical value 498.3668 Actual value 498.3676 NMR (δ, CDCfs); 0.8? (3H,t,
J=7Hz). 0.97 (3H, s), 1.03 (
3H,s). 1.18-1.36 (78, +I1).
1.41 (31,s), 1.45 (3H.s). 1
．． 56-1.76 (6H.*+), 1.78-1.94
(4H.+n), 2.16 (2H.t, J=7Hz)
12.36-2.42 (28, m). 2.55 (2H
, t, J=7Hz), 3.28(IH, d, J=7Hz
), 3.31 (211, dt, J=6Hz, 7Hz)
．． 3.44-3.65 (4HJ). 3.67 (
IH, d, J=1282). 4.06 (IH, S),
4.14 (2H, t, J=7Hz). 5.96-6.
02 (IH, a+). 6.90-7.04 (LH.+
w) 3 0 9 Example-59 3-N-tetradecanoylaminoprovil 3[N-
(2,2,5.5-tetramethyl-1,3 dioxane-
4-carbonyl)amino]propionate N-(3-hydroxybropyl)tetradecylamide 2
．． 87 g and 3-[N-(2,2.5,5tetramethyl-1,3-dioxane-4-carbonyl)aminocobropionic acid 2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 1.22 g of 4-(N,N-dimethylamino)pyridine in 301 g of toluene.
d and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, 310 water, then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain the title compound 4.63.
g (yield 88%) was obtained.

Properties: Oily IR (cm-', neat); ! lc. 0
1740+ 1656 Mass spectrometry Molecular formula i CzqHs
aNz Oa Theoretical value 526.3981 Actual value 526.3983 NMR (δ, cncf 3); 0.88 (3H,
t, J=7Hz), 0.98(3■,s), 1.0
4 (3■, s). 1.20-1.34 (15H, m),
1.42 (3H.s), 1.46 (3■, s). 1
．． 52-1.64 (4H.m), 1.84 (28, tt
, J=7Hz, 7Hz). 2.17 (2H, t, J=
7FIz). 2.36-2.44 (IH, m). 2
．． 56 (2H, t, J=7Hz), 3.29 (LH.
d. J=12Hz). 3.33 (2H.dt, J=6
Hz, 7Hz). 3.48-3.66 (4H.m).
3.68 (10.d, J=12Hz), 4.08 (L
H, s), 4.16 (2H, t, J=7Hz), 5
．． 92-5.96 (IH, m), 6.90-7.02
(IH.m) Example-60 3-N-hexadecanoylaminopropyl 3-[N-
(2.2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propionate N-(3-hydroxypropyl)hexadecylamide 3
．． 13 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid2. 5 9 g and dicyclohexyllupodiimide 2. 0 6 g and 4-(N,N-
dimethylamino)pyridine 1. 22 g was dissolved in 30 Ild of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate.

The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 5.48 g of the title compound (yield: 99%).
%) was obtained.

Properties: Oily IR (Cll-', .neat); I'cw
o 1740. 1658 mass spectrometry molecular formula; Ca+
HseNz Oh theoretical value 554.4294 actual value 554.4301 NMR (δ, CDCj2 s); 0.8B (3H
．． t, J=711z) IO. 98(3H,s), 1
．． 04 (3H, s), 1.21-1.36 (22H, m
). 1.43 (3H.s). 1.46 (3H, s).
1.56-1.98 (6H.m). 1.84 (2B,
tt, J=7Hz. 7Hz). 2.17 (28,t,
J=7Hz). 2.56 (2H, t, J=7Hz).
3.29 (11, d.J=12Hz). 3.32(
21, dd, J=7Hz, 6Hz). 3.67 (IH.
d, J=12Hz). 4.08 (IH.s). 4.
16 (2H.t.J=12Hz). 5.92-5.9
8 (IH.m). 6.92-7.04 (IH, 1) Example-61 3-N-octadecanoylaminopropyl 3-[N-
(2,2,5.5-tetramethyl-1.33 1 3 monodioxane-4-carbonyl)amino]propionate N-(3-hydroxypropyl)octadecylamide3. 42 g and 3-[N-(2,2,5,5tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 4-(N,N-
dimethylamino)pyridine 1. 22 g was dissolved in 301d of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 3.9 CIg (yield 67%) of the title compound 3 1 4 .

Properties: Oily IR (cn+-'+ neat); νc+0 1
738. 1652 mass spectrometry molecular formula; C33H62
Nt Oh theoretical value 584.4608 Actual value 582.4619 NMR (δ, CDC E s) i 0.88 (3F
I, t, J=7Hz) ,0.98(3H,s),
1.04 (3H, s), 1.20-1.36 (17H,
m), 1.42 (3H, s), 1.46 (3H, s)
, 1.54-1.96 (10H.m). 2.17 (3H
, t. J=7Hz). 2.56 (2H, t, J=7H
z) 3.28 (LH, t, J=12Hz), 3.33
(2H, dt, J=6Hz7}12). 3.44-3
．． 62 (4H, m), 3.67 (IH, d, J=12
Hz), 4.08 (LH, s), 4.16 (2H,
t, J=7Hz), 5.96-6.02 (IH, m),
6.92-7.04 (IH, m) Example-62 3-N-Linoleoylaminobyl 3-[N- (
2,2.5.5-tetramethyl-1,3-dioxane-
4-Carbonyl)amino]propionate N-(3-hydroxypropyl)linoleoylamide 3
．． 38 g and 3-[N-(2,2,5,5tetramethyl-1,3-dioxane-4-carponyl)amino]propionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 4-(NN-dimethylamino)pyridine 1. 2 2 g and 30 g of toluene
ml and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain the title compound in a yield of 67%.

Properties: Oily NMR (δ, Example 3-N (2. Oxanthate IR (01-1I mass spectrometry neat); νc-a 1740+ 165
4 molecular formula; C33HSllN2 0a Theoretical value 578,429,1 Actual value 578.4291 CDCj2 3); 0.89 (3H, t, J=7
Hz). 0.98 (311.s), 1.04 (
3H, s), 1.20-1.44 (17■, +n), 1
．． 43 (3H, s), 1.46 (3H, s),
1.52-1.76 (4H, m), 1.84 (2H, t
t, J=7Hz, 7Hz). 2.00-2.10(
6H, mL 2.17 (2H, t, J=7Hz>.
2.36-2.44(1}1,m). 2.56 (
2H,t,J=7■ZL 2.77(2■,t,.y
=7Hz), 3.29(LH, d, J=12Hz)
, 3.32 (2H, dd, J=6Hz, 7Hz).
3.46-3.64 (4■, m), 3.67 (LH
, d , J=12H2), 4.08 (1■, s)
, 4.16 (2■+1+J=12Hz), 5.28
-5.42 (IH, m). 5.92-6.00 (I
H,m), 6.94-7.02 (IH.m)63 Linolenoylaminobyl 3-[N2.5.5-tetramethyl-1.3-di4-carbonyl)amino]propione 3 1 7 N- (3-hydroxypropyl)linolenylamide 3
．． 35 g and 3- [N- (2, 2. 5. 5
-Tetramethyl-1,3-dioxane-4-carbonyl)amino]probionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 4-(N.
N-dimethylamino)pyridine 1. 2.2 g of the solution was dissolved in 30% of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 4.09 g of the title compound (yield: 71
%) was obtained.

Properties: Oily 3 1 8 IR (c+n-' Mass spectrometry NMR (δ, Example 1-N (2, oxanate neat); ν.-o 173B, 1652 molecules 2; C33H56N2 0h Theoretical value 576.4138 Actual value 576. 4126 CDC I!. 3); 0.97 (3■,t,J=
7Hz). 0.98 (3H, s). 1.05(
3H, s), 1.26-1.44 (12H.m), 1.
43(3}1,s), 1.46(3H,s),
1.53-1.74 (64m), 1.80-1.92 (
4H, m), 2.02-2.10 (2H, m), 2
．． 17 (21, t, J=7Hz). 2.34-2.4
2 (2H.m). 2.56 (2H, t, J=7Hz).
3.29 (IH, d, J=12Hz), 2.74-2
．． 86 (28, m). 3.28 (LH, d, J=1
2Hz)+3.32(2H, dd.J=6Hz.7Hz
), 3.42-3.66 (4H, m), 3.68
(IH, d, J=12Hz), 4.07 (18, s)
, 4.15 (2H, t, J=12Hz), 5.
26-5.44 (68.m). 5.90-6.00(
IH, m), 6.92-7.06 (Iff, m) 64 oleoylaminopropyl 3-[N 2,5.5-tetramethyl-1,3-di4-carbonyl)amino]probione If-( 4-Hydroxybutyl)oleoylamide 3.
54 g and 3-[N-(2,2,5.5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and f-(N,N-dimethylamino)pyridine 1. 22 g was dissolved in 30 d of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 5.05 g of the title compound (yield 85%).
I got it.

? Shape; Oily IR (cm-', neat); νc-o 17
40, 1662 mass spectrometry molecular formula; C34H6■N
206 Theoretical value 594.4608 Actual value 594.4618 NMR (δ, CDCj2 3); 0.88 (3H
, t, J=7Hz). 0.97 (3H, s). 1
．． 04 (3B, s). 1.20-1.40 (23H.m
). 1.43 (3■, s). 1.47 (3H.s).
1.50-1.80 (6H.II1), 1.86-2
．． 10 (3H.+n). 2.17 (2H.dt, J=
6Hz, 7Hz), 2.56 (28, t, J=6Hz
), 3.28 (IH, d, J=12Hz). 3.4
0-3.66 (2H, m), 3.69 (IH, d, J
=12Hz), 4.08(IN,s), 4.12<
2H, t. J=6Hz>. 5.30-5.40 (2H,
m), 5.48-5.56 (IH, n+), 6.90
-7.00 (IH, m) Example-65 4-(N-oleoylamino)butyl 3[N-(2.
4-dihydroxy-3.3-dimethyl-1-oxobutyl)amino]propionate 3 2 1 4-N-oleoylaminobutyl 3-[N-(2,2
,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propione} 0. 5 9 g
was dissolved in a mixed solvent of acetic acid 2 (l) and water (10 ml) and stirred overnight at room temperature. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain the title compound (0.5 0 g (yield 91%) was obtained.

Properties; Oily IR Ccm-'+ neat); νc=o 1
740, 1658 mass spectrometry molecular formula; C31H5
8N2 06 Theoretical value 554.4293 Actual value 554.4291 3 2 2 Nl'lR (δ, CDCj2 s) i 0.88
(3H, t, J=7Hz), 0.94 (3H, s
L 1.01 (3■, s), 1.18-1.42
(21H, m), 1.50-1.80 (64m).
1.90-2.12 (3H.m), 2.18 (2H, t
, J=7Hz), 2.45-2.57 (2H, m)
, 3.10-3.80 (8 Jl, m), 4.02 (
IN. …), 4.054.13 (11+.m).
4.18-4.26 (IH, m), 5.30-5
．． 41 (2H, m), 5.88-5.96 (IH.
m), 7.347.44 (1■+m) Example 66 5-(N-oleoylamino)bentyl 3[N- (
2,2,5.5-tetramethyl-1,3-dioxane-
4-Carponyl)amino]propionate N-(5-hydroxypentyl)oleoylamide3.
6 8 g and 3-[N- (2, 2, 5.5
-tetramethyl-1,3-dioxane-4-carponyl)amino]propionic acid2. 5 9 g and dicyclohexyllupodiimide 2. 0 6 g and 4-(N,
N-dimethylamino)pyridine 1. 22 g was dissolved in 30IIIL of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 4.99 g of the title compound (
A yield of 82%) was obtained.

Properties: Oily IR (cm-', neat); vc. o 1
738, 165B Mass spectrometry Molecular formula i C+sHaJ
z 06 Theoretical value 608.4764 Actual value 608.4764 NMR (δ, CDCI!.3); 0.8B (3■
, t, J=7Hz), 0.97 (3H, s), 1.
04 (311, s), 1.20-1.80 (26H, m
) 1.42 (3H, s), 1.46 (3H, s),
1.84-2.10 (4H, m) 2.15 (2B, t
, J=6Hz), 2.56(2H,t,J=6Hz
), 3.25 (IH, dt, J=6Hz, 6Hz),
3.29 (IH, d, J=12Hz). 3.40
-3.68 (4H, n+), 3.68 (IH, d,
J=12Hz), 4.08(IH,s). 4.10
(2H, t, J=12Hz), 5.30-5.40 (2
H. m). 5.48-5.54 (18, m), 6.90
-7.02 (IH, m) Example 67 5-(N-oleoylamino)hexyl 3[N- (
2.2,5.5-tetramethyl-1,3 dioxane-4
-carbonyl)amino]propionate 0 N (6 hydroxyhexyl) oleoyl 3 2 5 mido 3. 8 2 g and 3- [N- (2. 2.
5. 5-tetramethyl-1,3-dioxane-4
-carbonyl)amino]probionic acid2. 5 9 g
and dicyclohexylcarbodiimide2. 0 6 g and 4-(N,N-dimethylamino)pyridine 1. 2
2 g was dissolved in 30% toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain the title compound 2.8.
0 g (45% yield) was obtained.

Properties: Oily IR (cm-', neat); ν-o 174
0. 1656 mass spectrometry molecular formula i CsJ6aNz
Oh theoretical value 622.4920 Actual value 622.4923 NMR (δ, CDCj2 3); 0.88 (3H
, t, J=7Hz>, 0.97(3}1,s),
1.04 (3H, s). 1.20-1.54 (24H,
m), 1.43 (3H, s), 1.47 (3Ls),
1.56-1.70 (611, m), 1.90-2.
10 (4H, m), 2.15 (2H, t, J=7Hz
). 326 2.55 (2H, t, J=6Hz), 3.24 (IH
．． dt, J = 6Hz, 6Hz), 3.29 (11, d
, J=12Hz), 3.40-3.66 (2H, m)
, 3.68 (IH, d, J=12Hz). 4.08
(IH, s), 4.09 (2B, t, J=6Hz).
5.30-5.40 (2tl, m), 5.40-5
．． 50 (IH, m), 6.92-7.02 (LH, m)
Example 68 S-2-(N-oleoylamino)ethyl 3[N-
(2,2,5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanethionate N-(2-mercabutoethyl)oleoylamide3.
4 2 g and 3- [N- (2.2,5.5-tet?
Methyl-1,3-dioxane-4-carbonyl)amino]propionic acid2. 59 g and dicyclohexylcarbodiimide2. 0 6 g and 4-(N,N-dimethylamino)pyridine 1. 2 2 g and 3 toluene
0- and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 4.77 g (yield: 82%) of the title compound.

Properties: Oily IR (cn+-', neat); v io
1730+ 1656 mass spectrometry molecular formula ics■Hss
Nz Os S Theoretical value 582.4123 Actual value 582. 4095 NMR (δ, CDCI!.3); 0.88 (3H
, t, J=711z). 0.98 (30,s),
1.04 (3H.s), 1.20-1.40 (19H.s),
m), 1.43 (3H, s), 1.47 (3H, s)
, 1.58-1.70 (2H.m). 1.84-2.
10 (4H.n+), 2.17 (28, t.J=71
1z). 2.78-2.86 (2H.m), 3.05
(2H, t.J=6Hz). 3.29 (IH.d, J=
12Hz), 3.35-3.62 (5Lm). 3.
67 (IH, d, J=12Hz), 4.07 (IH
, s). 5.345.41 (28, m), 5.
93-6.02 (IH, m). 6.836.92(
IH, m) Example 69 S-2-(N-oleoylamino)ethyl 3-[N-
(2,4-dihydroxy-3,3-dimethyl-1-oxobutyl)amino]propanethionate S-2- (N-oleoylamino)ethyl 3- [
N-(2.2.5.5-tetramethyl-1.3-dioxane-4-carbonyl)amino]propanethionate 0. 58 g was dissolved in a mixed solvent of 20 d of acetic acid and 10 d of water, and stirred overnight at room temperature. After the reaction was completed, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to obtain 0.16 g of the title compound (
A yield of 29% was obtained.

Properties: Oily IR (cm-'+neat); vc-o 1
650 Mass spectrometry Molecular formula; CzJsJz Os S Theoretical value 542.3753 Actual value 542.3765 NMR (δ, CDCj! s); 0.8B (3H
．． t, J=7Hz) IO. 93 (3H, s). 1.
04 (3H, s), 1.15-1.40 (16H, m
), 1.504.70 (2H, m). 1.90-2.
06 (4H, m), 2.17 (2H.t.J=8Hz)
, 2.25-2.60 (6H, m), 2.70-2.
80 (IH, m). 2.82-2.98 (2H, m)
, 3.05-3.15 (IH.m). 3.30-3.
52 (6H, m), 4.01 (IH, s), 5.30
-5.42 (2H, m), 5.906.00 (ILb
rs). 7.22-7.32 (IH, brs) Example 70 N- [ (Is,2S) -2- (oleoylamino)cyclohexan-1-yl] -3- [N- (
2,3 3 0 2,5,5-tetramethyl-1,3-dioxane 4-carbonyl)amino]propanamide 1N-(2,2,5
．． 5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionic acid 745 ■N-(2-aminosyl-hexyl)oleoylamide 800 ■ and hydrochloric acid 1
-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (g) was dissolved in 50 ml of methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography to obtain the title compound 5.
04 mg (yield 34%) was obtained.

Properties; Oil optical rotation [α'Jゎ; -15. HC=1.0, C
}li l,)IR (cm~'+neat);
vc=o 1660+ 1642 mass spectrometry molecular formula;
CsbHb5Nz Os Theoretical value 619.4924 Actual value 619.4913 NMR (δ, CDCj2 3) i 0.8B (3H
, t, J=7Hz), 0.97(3H.s)+1
．． 04(3H,s), 1.15-1.37(24lI
, m), 1.43 (3H, s), 1.46 (3H, s
), 1.50-1.62 (2 ■ m). 1.68-1.
82 (2fl, m), 1.90-2.08 (6H, m
)2.11 (2H, t, J=7Hz), 2.28-2
．． 44 (2H, n+), 3.28 (IH, d, J=12
Hz), 3.36-3.48 (II, m), 3.55
-3.68 (3H, m). 3.69 (III, d, J
= 12Hz) 4.08 (LH, d, J = 11Hz),
5.29-5.40 (2H, m), 5.84 (LH, b
rs), 6.38 (IH, brs), 7.00 (I
H, t, J = 6 Hz) Example 71 rl- [(Is,2S) -2- (oleoylamino)cyclohexan-1-yl] -3-[N-( (
2R) -2,4-diacetoxy-3,3-dimethyll
-oxobutyl}amino]propanamide 1-N- {
(2R)-2,4-diacetoxy3,3-dimethyl-
1-oxobutyl}amino]propionic acid 187■ and (
Is, 2S) 1N=(2-aminocyclohexyl)oleoylamide 172■ and hydrochloric acid 1-ethyl-3-(3
-dimethylaminopropyl)carbodiimide g was dissolved in methylene chloride 5 (ld!) and stirred overnight. After the reaction was completed, the reaction solution was washed with water and dried over anhydrous sodium sulfate.
3 and the solvent was distilled off. The residue was purified by silica gel column chromatography to obtain the title compound 194 (yield 56%).

Properties; Oil optical rotation [α]D; -3.10 (C=1.0, CHC
ffis)IR (cm-', neat) ;νc
+o 1750, 1660 mass spectrometry molecular formula H Ci
6H6sNz Ow Theoretical value 663.4822 Actual value 663.4833 NMR (δ, CDCI!.3); 0.88 (3H
, t, J = publication z), 1.03 (311, s), 1
．． 08 (3H, s). 1.18-1.39 (241{
．． m). 1.07-1.83 (2H, m). 1.92
-2.09 (6H, m), 2.08 (3H, s). 2
．． 14 (2H, t.J=7Hz). 2.20 (3H,
s), 2.32 (2H, t, J=7Hz), 3.2
8-3.40 (IH, m), 3.49-3.59 (2
H. m), 3.61-3.74 (IH, m), 3.
82 (IH, d, J = 12Hz), 4.04 (18, d
, J=12Hz), 4.09(IH,s), 5.29
-5.40 (28, m), 5.79 (IH, d, J=8
Hz). 6.19 (IH, d, J=8Hz), 7.0
3 (IH, t, J=6■2) Example-72 3 3 4 N [2 (oleoylamino) cyclohexane 1 yl] 3 [N { (2R) 2. 4-diacetoxy3. 3 dimethyl 1 oxobutyl} amino]propanamide [B] 3 [N (2, 4 diacetoxy 3, 3 dimethyl-1-oxobutyl) amino] propionic acid 1
．． 01g and N-(2-aminocyclohexyl)oleoylamide 1. 26 g and 1-ethyl 3-(3
-dimethylaminopropyl)carbodiimide 1.91g
was dissolved in 50 mρ of methylene chloride and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography, and the title compound was converted into two diastereomers A [N- [ (IR,2R) -2
-(oleoylamino)cyclohexan-1-yl]-3-[N{ (2R)-2.4-diacetoxy-3.3
-dimethyl-1-oxobutyl}amino]propanamide] and B [N- [(Is,2S) -2- (oleoylamino)cyclohexan-1-yl]3-[N
- ((2R)-2.4-diacetoxy3.3-dimethyl-1-oxobutyl}amino]propanamide) 603■ (yield 28%) and 714■ (yield 33%), respectively.
) was obtained.

A Properties; Oil optical rotation [α] n; −32.0 (C・1.0,
CHi3)IR (cm-', neat);
vc. o 1750+ 1660 mass spectrometry molecular formula;
CsrHbsN30+Theoretical value 663.4822 Actual value 663.4834 NMR (δ, CDCj2 3); 0.88 (3H,
t, J=7Hz), 1.08 (311,s), 1.
10 (3H, s). 1.21-1.38 (24H, l
I1), 1.46-1.65 (2H, m), 1.69
-1.79 (2H, m). 1.88-2.08 (6H,
n+), 2.08 (38,s). 2.13(2H,t
, J=7Hz), 2.14-2.26(IH, n+
), 2.16(31,s), 2.23-2.42(
IH, m). 3.06-3.16 (IH, m). 3.5
6-3.79 (3H, m), 3.90 (IH, d, J
=lIHz)4.07(1■,d,J=11Hz),
4.80 (IH.s), 5.295.42 (10, m
), 5.69 (IH, d, J=8Hz), 6.56
(IH, d, J=8Hz). 7.41 (IH, t, J
= 6 Hz) B Properties; Oil optical rotation [αL; -3.10 (C = 1.0, CHi
s)IR (Cll1-', neat); vc
．． o 1750+ 16603 3 7 Mass spectrometry Molecular formula i C3JasNi 0? Theoretical value 6
63.4822 Actual value 663.4833 NMR (δ, CDCj! 3) i 0.88 (38
, t, J=7Hz), 1.03(3H,s), 1
．． 08 (3H, s), 1.18-1.39 (24H,
m), 1.07-1.83 (2H, m), 1.92-
2.09 (6H, m), 2.08 (3H, s), 2.
14 (2H, t, J=7Hz), 2.20 (3H, s
), 2.32 (2H, t, J=7Hz), 3.28
-3.40 (IH, m), 3.49-3.59 (2H
, m), 3.61-3.74 (LH, m), 3.8
2 (IH, d, J = 12Hz), 4.04 (IH, d
, J=12Hz), 4.09(IH,s), 5.2
9-5.40 (2Hm). 5.79 (1■.d, J=
8Hz), 6.19 (LH.d, J=8Hz), 7
．． 03 (IH, t, J = 6Hz) Example-73 N- [(IR,2R)-2- (oleoylamino)cyclohexan-1-yl] -3- [N-{ (
2R)-2,4-dihydroxy-3,3-dimethyl1-
oxobutyl}amino]propanamide 3 3 8 AcO Ac0 N- [(IR,2R)-2- (oleoylamino)cyclohexan-1-yl] -3- [N-{(2
R)-2,4-diacetoxy-3,3-dimethyl-1-
Oxobutyl)amino]propanamide was dissolved in 380 μl of methanol (10 w1), and while stirring at room temperature, 0.5 μl of a 1N aqueous solution of caustic soda was added, and the mixture was stirred for 2 hours. After the reaction was completed, the solvent was distilled off under reduced pressure, extracted with ethyl acetate, the organic layer was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography to obtain the title compound 293 (yield: 89%).

Properties: Oil optical rotation [α] n; +34. DC=1.0,
CHCA 3) IR (cm-', neat);
vc. o 1642 mass spectrometry molecular formula; C33H6
1N3 0S theoretical value 579.4611 actual value 579.4596 CDCl s); 0.8B (3H. t.J=7
Hz), 0.95 (3H, s). 1.04 (3H
, s). 1.17-1.38 (24H, m), 1.4
9-1.62 (2H, +w). 1.73-1.82(
2H, m), 1.93-2.08 (61, m), 2.
14 (2H, t, J=7Hz). 2.31-2.45(
2H. m). 2.52-2.86 (2B, m), 3.
44-3.73 (68, m), 3.98 (IH, s)
, 5.28-5.40 (2H, m), 6.08 (1
■, brs), 6.63 (IH, brs). 7.3
4(In,t,J=6Hz) Example-74 N- [(Is,23)-2- (oleoylamino)cyclohexan-1-yl] -3- [N- {
(2R)-2,4-dihydroxy-3,3-dimethyl N
MR (δ, ■ Oxoptyl}aminocopropanamide N- [(is,2s)-2- (oleoylamino)
cyclohexan-1-yl]-3-[N{(2R)-2
．． 4-Diacetoxy-3,3-dimethyl-1-oxobutyl}amino]propanamide 485 ■ Methanol 10
Dissolve in WI1 and add 0.0% of 1N caustic soda aqueous solution while stirring at room temperature. 57 was added and stirred for 2 hours. After the reaction is complete,
The solvent was distilled off under reduced pressure, extracted with ethyl acetate, the organic layer was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off.

The remaining product 341 was purified by silica gel column chromatography to obtain the title compound 410 (yield 97%).

Properties: Oil optical rotation [α] n: -0.60 (C=1.0,
CIC 12 3) IR (co+-', neat
); vc-o 1644 mass spectrometry molecular formula; C
33H61N3 0S Theoretical value 579.4611 Actual value 579.4603 NMR (δ, CDC l 3) i 0.88 (3■
, t, J=7Hz), 0.94 (3■, s), 1.
05 (3H.s). 1.16-1.38 (24H, m
). 1.46-1.62 (2H, m). 1.71-1
．． 82 (2H, n+), 1.87-2.07 (6H.l
l1). 2.12 (2H, t, J=7Hz). 2.3
2-2.44 (IB, m). 2.48-2.58 (I
H, n+). 2.63-3.05 (2H.o+). 3
．． 18-3.29 (IH.m). 3.46(IH+d
, J=11Hz). 3.51 (IH, d,
J=11Hz). 3.55-3.73 (2H.m),
3.86-3.99 (IH, m). 4.12 (IH,
s), 5.29-5.41 (2H, m), 5.99 (
IH, d, J = 8 Hz), 7.02 (It{, d, J
=8Hz), 7.117.19 (IH, m) 34 2 Example-75 N-[2-(oleoylamino)cyclohexane 1
-ylco-3- [N- (2,4-diacetoxy-3
,3-dimethyl-1-oxobutyl)amino]propanamide [Acod I-1 [N-(2.4-diacetoxy3.3-
dimethyl-1-oxobutyl)amino]probionic acid 1
．． 51 g of (IR.2R)-N-(2aminocyclohexyl)oleoylamide and 1.91 g of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride were dissolved in 50 g of methylene chloride. Stir overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography to give the title compound 2.
Species diastereomer A [N- [ (IR,2R)
2-(oleoylamino)cyclohexane-1yl]
-3- [N- { (2R)-2.4-diacetoxy-3.3-dimethyl-1-oxobutyl}amino]propanamidoco and B[N-[(IR2R)-2-(oleoylamino)cyclohexane -l-il] -3-
[N-((2R)-2.4-diacetoxy-3,3
848 g (28% yield) and 1.00 g (33% yield) of -dimethyl-1-oxobutyl}amino]propanamide were obtained, respectively.

[A] Properties; Oil optical rotation [αL; -32.0 (C=1.0+CHC
1s) IR (cm-', neat); vc-
o 1750. 1660 mass spectrometry molecular formula H C3q
HbsNsO? Theoretical value 663.4822 Actual value 663.4834 NMR (δ, CDC13); 0.8B (3H,
t, J=7FIz). 1.08 (38,s). 1.
10 (3H, s). 1.21-1.38 (24H, m
), 1.46-1.65 (2H.m), 1.69-1
．． 79 (2H.m), 1.88-2.08 (6H.m)
, 2.08 (3H, s), 2.13 (28, t, J=
7Hz), 2.14-2.26 (IH, m), 2.
16 (3H, s), 2.23-2.42 (IH, m)
．． 3.06-3.16 (IH, m), 3.56-3.7
9 (3H, m). 3.90 (IH, d, J=11Hz
), 4.07 (1■.d.J=11Hz), 4.80
(ILs), 5.295.42 (1■.m). 5.
69 (IH.d, J=8Hz). 6.56(LH,d
, J=8Hz). 7.4H1■, t, J=6Hz
) [B] Properties; Oily 3 4 5 Optical rotation [α] o: +2.04 (C.・1.0
, Cl(J'3)IR (cm-'.neat)
: v. -o 1750,1660 Mass spectrometry Molecular formula H C3J6sNz Oq Theoretical value 663.482
2 Actual value 663.4833 NMR (δ, CDC1s); 0.8B (30,
t, J=7Flz), 1.03 (3H, s), 1.
08 (3H, s). 1.18-1.39 (24Lm)
, 1.07-1.83 (2H, m), 1.92-2.
09 (68, m), 2.08 (3H, s), 2.14
(2H, t, J=7Hz), 2.20 (3H.s).
2.32 (2H, t, J=7Hz), 3.28-3
．． 40 (IH, m). 3.49-3.59 (2H, n
+), 3.61-3.74 (IH.m). 3.82
(IH, d, J=12Hz), 4.04 (11.d,
J=12Hz). 4.09 (IH, s), 5.29
-5.40 (2H, m), 5.79 (18, d, J=
8Hz), 6.19 (IH, d, J=8Hz), 7
．． 03 (IH, t, J = 6Hz) Example-76 N- [2-(oleoylamino)cyclohexane 1-
ylco-3- [N- (2,4-diacetoxy-3.
3-dimethyl-1-oxobutyl)amino]propanamide 3 4 6 [A] dl-3- [N- (2.4-diacetoxy 3.3
-dimethyl-1-oxobutyl)amino]brobionic acid 1. 4 4g, (Is,2S)-N-(2aminocyclohexyl)oleoylamide] 1.80g and 1-ethyl-3-(3-dimethylaminobrobyl)carbodiimide hydrochloride 1.91g were added to 50ml of methylene chloride. Dissolved and stirred overnight. After the reaction was completed, the reaction solution was washed with water, dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography, and the title compound was divided into two diastereomers A [N-[(I
B [N[(Is,2S)-
2-(oleoylamino)cyclohexan-1-yl]
-3- [N- ((2S)2.4-diacetoxy-3.3-dimethyl-1oxobutyl}amino]propanamide], respectively, at 859 μ (yield 29%) and 0.80
g (yield 27%) was obtained.

[B] Properties; Oil optical rotation [α] b: -32.0 (C・1.0,
CHCji! 3) IR (cm-', neat)
; l'(=Q 1750, 1660 mass spectrometry molecular formula; C37H6SN307 theoretical value 663.482
2 Actual value 663.4834 NMR (δ, CDC (1 3); 0.88 (3
H, t, J=7Hz), 1.08(3H,s),
1.10 (3H, s), 1.21-1.38 (24
1+, m), 1.46-1.65 (2H, m). 1.
69-1.79 (2H, m). 1.88-2.08 (6
■, m), 2.08 (3H, s), 2.13 (2Ht
, J=7Hz), 2.14-2.26 (11, m).
2.16 (3H, s), 2.23-2.42 (IH
, m), 3.06-3.16 (IH, m) 3.56-3
．． 79 (3H, +w). 3.90 (1■, d, J
=lIFlz)4.07(LH,d,J=11Hz),
4.80 (LH, s), 5.295.42 (LH,
m), 5.69 (IH, d, J=8Hz). 6.5
6 (LH, d, J=8Hz), 7.41 (LH, t.
J=6Flz) Example-77 (IR,2R)-2-(oleoylamino)cyclohexan-1-yl 3 [N-(2,2.5.5-tetramethyl-1.3-dioxane-4- carbonyl)amino]probionate 3 4 9 (IR,2R)-1 (N-oleoylamino)cyclohexanol 3. 7 9 g and 3- [N- (2,
2.59 g of 2,5.5-tetramethyl-1,3-dioxane 4-carbonyl)amino]brobionic acid and dicyclohexylcarbodiimide 2. 0 6 g and 4- (
N. 1.22 g of N-dimethylamino)pyridine was dissolved in 30 mR of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate.

The solvent was distilled off, and the remaining 350 residue was purified by silica gel column chromatography to obtain 3.27 g (yield: 53%) of the title compound.

Properties; Oil optical rotation [α]n; +26.2 (C=1.0.CH
C#3) IR (cm Ichito, neat); v.
-o 1736, 1654 mass spectrometry molecular formula; C36
■b4NZ 06 Theoretical value 620.4764 Actual value 620.4759 NMR (δ, CDC l 3); 0.88 (38
, t, J=7Hz), 0.99 (3Hs), 1.
04 (3H, s), 1.07-1.39 (24H, m
), 1.43 (3H, s), 1.48 (3■, s),
1.50-1.83 (4H, m), 1.92-2.1
7 (6H, n+), 2.10 (211, t, J=7Hz
)2.51 (2H.t, J=6Hz), 3.32-3
．． 43 (1B, m), 3.57-3.68 (IH, m)
, 3.69 (LH, d, J=12Hz). 3.83-
3.95 (IH, m), 4.08 (IH, s). 4.
64 (IH, td, J=11Hz, 5Hz), 5.2
8-5.40 (IH m) 5.74 (IH, d, J=
8Hz), 6.95 (LH, t, J = 6Hz) Example-78 (Is, 23) -1(oleoylamino)cyclohexan-1yl 3-rN- (2, 2, 5, 5-tetramethyl (Is,2S)-2-(N-oleoylamino)cyclohexanol3. 7 9 g and 3-[N-(2,
2,5.5-tetramethyl-1,3-dioxane = 4-
2.59 g of dicyclohexylcarbodiimide and 4-(N,
N-dimethylamino) and 1.22 g of lysine were dissolved in 30 d of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 3.52 g of the title compound (yield 57%).
I got it.

Properties: Oil optical rotation [α] n; +14.3 (C=1.0,
C41C# 3) IR (cm-', neat)
; l/c+l+ 1734. 1654 mass spectrometry
Molecular formula; C+6H6Jz Oh theoretical value 620.47
64 Actual value 620.4777 NMR (δ, CDCl3); 0.88 (3H
, t. J=7Hz). 0.96 (3H, s),
1.04 (3H.s). 1.06-1.38 (24H
, m). 1.43 (3FI, s). 1.47 (38,
s), 1.48-1.80 (4H, m). 1.92-
2.17 (6H.m), 2.10 (2H, t, J=7H
z), 2.51 (2H, t, J=6Hz), 3.28
(IH, d, J=12Hz)+3.45-3.57(2
H, m), 3.69 (1}1, d, J=12Hz),
3.82-3.93 (LH.m). 4.08 (IH,
s), 4.64 (IH, td, J=11Hz, 5Hz)
, 5.79 (LH, d, J=8Hz). 3 5 3 6.91 (LH, t, J=6Hz) Example-79 (IR, 2R) -2- (stearoylamino) clohexan-1-yl 3 [N-(2,2.5-tetramethyl -1,3-dioxane-4rubonyl)amino]probionate 5. Ka(IR,2R) -2- (N-stearoylamino)
3.81 g of cyclohexanol and 3-[N-(2,2
．． 5.5-tetramethyl-1,3-dioxane 2.59354 g of 4-carbonyl)amino]probionic acid and 2.54 g of dicyclohexylcarbodiimide. 0 6 g
and 4-(N,N-dimethylamino) and lysine 1.22
g was dissolved in 30 ml of toluene and heated under reflux overnight.

After the reaction was completed, it was cooled, the precipitate was removed, and the organic layer was diluted with 1N hydrochloric acid,
It was washed with water and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain the title compound 2.82.
g (yield 45%) was obtained.

Properties: Melting point: 69.1-70.2 Optical rotation: α
”. ; +25.8(C=1.0+CHC It
3) IR (am-', neat); l/c
=o 1734, 1660. 1646 mass spectrometry molecular formula; C+6tlaJg Oh theoretical value 622.49
20 Actual value 622.4930 NMR (δ, CDCl3): 0.88 (3H
, t, J=7}1z), 0.99(3H,s)
1.04 (3H, s), 1.11-1.34 (32H
, m). 1.43 (3H, s), 1.48 (3B, s
), 1.50-1.83 (4N, m), 1.92-2
．． 18 (2H, m), 2.10 (211, t, J=7t
lz). 2.51 (2H, t, J=6Hz), 3.2
9 (10, d, J=12Hz). 3.31-3.42(
IH, m), 3.57-3.68 (IH, m), 3
．． 69 (18, d, J=12Hz), 3.83-3
．． 95 (IH, m) 4.08 (IH, s), 4.6
4 (1B, td, J=111{z, 5Hz), 5.74
(IH, d, J=8Hz), 6.95 (LH, t,
J=6Hz) Example-80 (Is.2S)-2- (linoleoylamino)cyclohexan-1-yl 3-[N- (2,25,5-tetramethyl-1.3-dioxane-4carbonyl) ) Aminocoprobionate? Hexanol 3. 7 7 g and 3- [N-
(22.5.5-tetramethyl-1,3-dioxane 4
-carbonyl)amino]probionic acid 2.59 g and dicyclohexyllupodiimide 2. 0 6 g and 4-
(N,N-dimethylamino)pyridine (1.22 g) was dissolved in 30% of toluene and heated under reflux overnight. After the reaction was completed, the mixture was cooled and the precipitate was removed, and the organic layer was washed with 1N hydrochloric acid, water, and then saturated brine, and dried over anhydrous sodium sulfate. The solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 2.72 g (yield: 44%) of the title compound.

Properties; Oil optical rotation [α] n; +13.5 (C=1.0,
CHCji! 3) IR (cm-', neat)
; l7cmG 1736. 1654 mass spectrometry
Molecular formula i CiJl6■N206 Theoretical value 618.46
07 Actual value 618.4612 NMR (δ, CDCj! 3); 0.89 (3H
．． t, J=7Hz), 0.96 (3Hs), 1.0
4 (3H.s), 1.11-1.39 (18■, m)
,3 5 7 1.43(311,s), 1.47(3H,s)+
1.51-1.81 (4H, m), 1.95-2.1
8 (6■, m), 2.10 (2H, t, J=7Hz),
2.50 (2■, t, J=6Hz), 2.77 (LH
, t, J=6Hz), 3.28(LH, d.J=12H
z), 3.46-3.57 (28, m). 3.69 (
IH, d, J=12Hz), 3.32-3.43(L
H, m), 4.09 (LH, s), 4.64 (IH,
td+J=11Hz, 5Hz)+5.28-5.43(
4H, m), 5.80 (IH, d, J=8Hz), 6
．． 91 (IH, t, J=6Hz) 3 5 8 Reference Example 22 (IS, 2S)-2-(N-benzyl-N-hexyl-rubamoyl)aminosichexanol (13,
2S) -2-Aminocyclohexanol 345Mlg
And 424 ■ of sodium carbonate to 10 m of ethyl acetate! ! ．．
The mixture was dissolved in 10 mj2 of water, and a solution of 470 ml of phenyl chlorocarbonate dissolved in 5 nffi of ethyl acetate was added dropwise to the mixture under water-cooling and stirring, and the mixture was stirred for 2 hours after the dropwise addition was completed.

After the reaction was completed, the aqueous layer was separated and extracted with ethyl acetate, and the organic layers were combined and washed with saturated brine. After drying over anhydrous sodium sulfate, the solvent was distilled off, and N-penzylhexylamine 1. Add 15 g, 100″
The mixture was stirred at C for 1 hour. After the reaction was completed, the residue was purified by silica gel chromatography to obtain 866 mg of the title compound.
(yield 87%).

NMR (δ, CDCj23) 0.87 (3N, t, J=7}1z), 0.96-2
．． 08 (1611, m), 3.15-3.54 (4H
m), 4.25 (LH.d, J=6Hz) 4.47 (
2H, s), 4.67 (1}t, d, J=3Hz).
7.20-7.41 (5H, m) Reference Example 23 Benzyl 2-(N-(2.4-dihydroxy-3.3
dimethylbutanoyl)amine]acetate pantoyl lactone 1 3. 0 g and glycine 8.3 g and 85%
Potassium hydroxide was dissolved in 100 ml of methanol and heated under reflux for 3 hours. The solvent was distilled off from the reaction solution under reduced pressure. After drying the residue, dimethylformamide 150mj2
Dissolve in benzyl bromide 1 8. 8 g was added and stirred at room temperature for 20 hours.

The reaction solution was evaporated under reduced pressure, and the residue was dissolved in water and extracted with ethyl acetate. The organic layer was washed with water and then with saturated saline,
After drying over anhydrous sodium sulfate, the solvent was distilled off, and the residue was purified by silica gel column chromatography to obtain 12.8 g (43%) of the title compound.

NMR (δ, CDCl3) 0.95 (3H, s), 1.06 (3H, s), 2
．． 73 (2H, br-s), 3.51 (IH, d, J=
l. IHz), 3.56 (IH, d, J=11Hz)
, 4.03-4.21 (2H.m), 4.09 (IH.
, s), 5.19 (2H.s). 7.23-7.28
(In, m), 7.33-7.42 (5H, II1)
Examples 81 to 164 The following compounds were produced in the same manner as in Example 1.

Example 81 Compound name: (R)-1-methyl-2-oleoylamino
Ethyl 3-(N- 2.2,5.5-tetramethyl-
1,3-dioxane-4-carbonyl)a361mino]probionate Structural formula: Molecular formula: C33H6. N206 Molecular weight 7 580.85 Mass spectrometry calculated value 7 580.4451 Actual value: 58
0.4448 Melting point ("C): oil Optical rotation: [α)" 31.1° (C=1.O CH
l3) IR(ν++eat+CIII-'): 3
332, 2932, 2860. 1740. 16
60NMR (δ, CDCffii): 0.88 (
3H,t,J=7Hz), 0.99(3H,s).
1.02 (3H, s) 1.21-1.38 (23H, m
). 1.43 (3H, s), 1.47 (311, s
), 1.55-1.69 (28, m), 1.91-2
．． 08 (4H, m), 2.20 (2H, t, J=7Hz
), 2.44-2.62 (2H, m), 3.29 (I
I{,d,J=12flz). 3.30-3.53(
3H, m), 3.65-3.78 (IH, m), 3.
68 (LH, d, J=12Hz), 3 6 2 4.07 (38, s). 4.92-5.03 (IH
, m). 5.29-5.40 (2H, m). 6.3
0-6.38 (1 fl.m). 6.91 (11, t,
J=6Hz) Example 82 Compound name: (S)-1-methyl-2-oleoylamino
Ethyl 3-(N-(2,2,5.5-tet)
lamethyl-1,3-dioxane-4-carbonyl)amide
] Propionate structural formula: Molecular formula: Cs3HboNtOb Molecular weight: 580.85 Mass spectrometry calculated value 7 580.4451 Actual value: 58
0.4458 Melting point ("(:) :oil Optical rotation: [α)" 21.6° (C=1.O CH
Cj23) IR (v783 CIII~'): 3332, 2932, 2860. 1738. 1
662NMR (δ, CDCl3): 0.88
(3H, t, J=7Hz). 0.97 (3H, s)
, 1.04 (38,s), 1.20-1.37 (2
3H, m), 1.43 (3H, s), 1.47
(3H, s) 1.56-1.68 (2H, n+),
1.91-2.08 (1, m), 2.20 (2H, t.
J=7Hz), 2.44-2.62(2H, m)3
．． 26-3.35 (IH.m), 3.28 (IH,
d, J=12Hz), 3.42-3.58 (2H, m)
, 3.64-3.75 (IH, m), 3.70 (I
H. d, J=12Hz), 4.07 (IH, s),
4.93-5.03 (LH, m). 5.28-5.
41 (2H, m), 6.27-6.34 (II, m),
6.88-6.96 (IH, m) Example 83 Compound name: (IS,2S)-2- (oleoyl
Mino) cyclopentan-1-yl 3-( N - (
2.2.55-tetramethyl-1,3-dioxane-4
-carbonyl)amino]propionate Structural formula: (S,S)? Child formula: C3sHb■NzOh Molecular weight: 606.89 Mass spectrometry calculated value: 606.4607 Actual value: 60
6.4617 Melting point (C): oil Optical rotation: (α) 2324.5° (C=1.0 CH
Cj2i) I R (V n., it+ Cffl-
'): 3324, 2932, 2860, 173
6. 1654NMR (δ, CDCfs): 0.88 (3H, t, J=7Hz), 0.96 (3H
,s), 1.04(3■+S)+1.20-1.48
(22H, m), 1.43 (3H, s), 1.46
(3H, s). 1.52-2.09 (9H, m), 2
．． 13 (2H, t, J=7Hz), 2.18-2.22
(LH, m), 2.54 (2H, t.J=6Hz).
3.28 (LH, d, J=12Hz), 3.48-3
．． 59(2■+m)+3.69(LH.d,J=12H
z), 4.08 (IH, s), 4.08-4.19 (
IH, m), 4.92-5.01 (IH.m). 5.
29-5.40 (2H, m), 5.72 (IH, d,
J=7Hz), 6.98(IFI.t, J=6Hz>
Example 84 Compound name: (IR,2R)-2- (oleoyl
Mino) 36 5 cyclopencun-1-yl 3 - (N - (2
,2,5.5-tetramethyl-1,3-dioxane-4
-Carbonyl)amino]propionate Structural formula: (R.R) Molecular formula: C3SH62N206 Molecular weight: 606.89 Mass spectrometry calculated value: 606.4607 Actual value 7 60
6.4614 Melting point (C): oil Optical rotation: [α)” 14.9° (C=1.0 CH
CI! ．． 3) I R (El nast+ CIl1
-') '332B, 2932. 2B60, 17
40. 1656NMR (δ, CDCI!.s)
:0.88(3H,t,J=7Hz), 0.99(3
}1, s). 1.04(3Fl,s), 1.21-1
．． 47 (22■, m), 1.43 (3B, s), 1
．． 46 (3H, s), 1.53-2.12 (9B, m)
, 2.13 (21+.t, J=7Hz), 3 6 6 2.18-2.31 (IH.m), 2.54 (2H
, t, J=6Hz), 3.28(IH, d, J=12H
z), 3.36-3.49 (1B, m), 3.58
-3.69 (IH m), 3.69 (18, d, J
=12Hz), 4.08(IH,s), 4.09-
4.20 (IH, m), 4.95-5.02 (LH, m
), 5.29-5.40 (2H.m), 5.72 (
18, d, J = 7Hz), 7.02 (IH, t, J
=6tlz) Example 85 Compound name: (Z)-4-oleoylamino-2-butenyl
3-(N-(2,2,5.5-tetramethyl1
．． 3-Dioxane-4-carponyl)amino]propio
Nate structural formula: Molecular formula: C34HaoNzOb Molecular weight: 592.80 Mass spectrometry calculated value 7 592.4451 Actual value 7 59
2.4424? Point ("C): oil Optical rotation: [α)"22.2" (C=1.0
CICI23) IR( ν ■aat+ Cm 1
Tsuta) :3336. 2932. 2B60,
1740. 1660NMR (δ, CDCI
! ．． 3): 0.88 (3H. t, J=7Hz), 0.90 (
3H,s). 1.04 (3H, s), 1.20-1
．． 38 (20H.m), 1.43 (3H.s),
1.46 (3H.s). 1.54-1.69 (211
, m), 1.91-2.08 (4H, m) 2.17
(2■, t, J=7Hz). 2.57(2H,t,
J=6Hz), 3.28 (IH, d, J=12Hz).
3.42-3.67 (2H, m). 3.69 (IH
, d, J=12Hz), 3.97(2■, dd,
J=6Hz+6Hz) +4.08(IH,s),
4.70 (2H.d, J=6Hz)+5.29-5
．． 40 (28, m), 5.59-5.80 (3H,
m). 6.88-6.96 (1■+m) Example 86 Compound name: (R)-2-methyl-2-oleoylamino
Ethyl 3-(N-(2.2,5.5-tetramethyl-
1.3-dioxane-4-carbonyl)amino]propyl
Onate structural formula: (R) Molecular formula: C+JaoNz06 Molecular weight: 580.85 Mass spectrometry calculated value: 580.4451 Actual value 7 58
0.4458 Melting point ("C): oil Optical rotation: [α)"31.0' (C=1.0
CHCf. )IR(νllaat+ Clfl-')
:3324, 2932. 2860. 1740.
1660NMR (δ, CDCjh)' 0.88 (3H, t, J=7Hz). 0.98 (3H
, s). 1.04 (3Fl.s), 1.18 (3■,
d, J=6Hz), 1.23-1.39(20H, m
), 1.43 (3H, s), 1.47 (3H, s).
1.57-1.68 (2}1, m), 1.92-2.
08 (4Lm). 2.16 (2H, t, J=7Hz)
, 2.58 (2H.t, J=6Hz), 3.28 (I
H, d, J = 12Hz). 3.57 (2H, dt, J=
6+lz, 6Hz). 3.69 (LH.d, J=12
Hz), 4.03-4.14 (2H, m), 4.07
(IH, s), 3 6 9 4.26-4.37 (IH m), 5.29-5.
40 (2H, m), 5.84 (IH, d.J=8Hz)
．． 6.98 (IH, t, J=6Hz) Example 87 Compound name: (S)-2-methyl-2-oleoylamino
Ethyl 3-(N-(2,2,5.5-tetramethane)
Chil-1,3-dioxane-4-carponyl)amino]
Probionate structural formula: (S) Molecular formula: 033■60N! 06 Molecular weight 7 580.85 Mass spectrometry calculated value: 580.4451 Actual value: 58
0.4442 Melting point ("C): oil Optical rotation: [α)"13.1' (C=1.O
CHCffi3)IR (1' neit+ CIl
l-') :3320,2932.2860.174
4.1654 3 7 0 NMR (δ, CDCj2:+): 0.88 (3H, t.J=7Hz), 0.97 (3
H. s), 1.03 (3H, s), 1.16 (3H
, d, J=6Hz), 1.21-1.39 (20H
, m), 1.42 (3H, s), 1.47 (3H,
s), 1.54-1.68 (2H, m), 1.92
-2.08 (48, m), 2.17 (2B, t, J
=7Flz), 2.58 (2H, t, J=6Hz),
3.28 (LH, d, J=12Hz). 3.49-3
．． 67 (2H, m), 3.69 (LH, d, J=1
211z), 4.05 (II, dd, J=11Hz, 4
Hz), 4.07 (IH, s), 4.13 (LH,
dd, J=11Hz, 5Hz), 4.22-4.3
6 (LH, m), 5.29-5.42 (28, m).
5.92 (IH, d, J = 8Hz), 6.92 (LH
．． t, J=5Hz) Example 88 Compound name: (E)-4-oleoylamino-2-butenyl
3-(N-(2,2,5.5-tetramethy)
13-dioxane-4-carponyl)amino]propyl
Onate structural formula: ? Child type: C34■,. N206 Molecular weight: 592.86 Mass spectrometry calculation value: 592.4451 Actual measurement {! :
592.4459 Melting point ("(:) :oil Optical rotation: [α)"22.1"' (C=1.O
CRCI! ．． 3) I R (1/,,@■4 Cl
ll-') :3328. 2932, 2860,
1740. 1660NMR (δ, CDCj!3)
: 0.88 (3H, t, J=7Hz), 0.96 (3H
, s), 1.04 (3H, s), 1.21-1.38
(20H, m), 1.43 (3H, s), 1.46
(3H, s). 1.56-1.69 (2Lm), 1.
91-2.08 (4H, m) 2.18 (2■, t, J=
7}1z), 2.58 (2H, t, J=6Hz), 3
．． 28 (2H, d, J=12Hz), 3.41-3.
68 (2Lm), 3.69 (IH.d, J=12Hz)
, 3.90 (2H+dd, J=6Hz+6Hz), 4
．． 08 (IH, s), 4-57 (2H, d+J=6H
z), 5.28-5.41 (2H, m), 5.52-
5.62 (IH, m). 5.65-5.83 (2H, m
), 6.95 (LH, t, J = 6Hz) Example 89 Compound name: 4-oleoylamino-2-butynyl 3-[
N-(2,2,5,5-tetramethyl-1,3dioxa
4-carbonyl)amino]propionate Structural formula: Molecular formula: C34HSllN206 Molecular weight: 590.85 Mass spectrometry calculated value: 590.4294 Actual value: 59
0.4279 Melting point (C): oil Optical rotation: [α)” 21.2°IR (ν,, +1at+ cm-'): 3320,
2932. 2860. 1748. 1662NMR
(δ, CDCffi, l): 0.88 (3H,
t, J=7Hz) ,1.21-1.39(20H
, m). 1.58-1.72 (2H, +w). (c=1.o
cock 3) 0.97 (3■, s), 1.04 (3H, s), 1
．． 43 (3H, s), 1.47 (3B, s). 1.
92-2.08 (4H, *). 3 7 3 2.18 (2H, t, J=7Hz), 2.61 (2
H, t, J=6Hz). 3.28 (2H d, J=12
Hz), 3.42-3.68 (2H.m), 3.7
0 (IH, d, J=12Hz). 4.08 (1B,
s), 4.08-4.11 (2H, m), 4.69
-4.72 (2H, m) 5.29 - 5.42 (2H, m
), 5.68-5.78 (LH, m), 6.96 (
1}1. t. J=5Hz) Example 90 Compound name: (R)-2-oleoylamino-2phe
Nylethyl 3-[N-(2.2,5.5-tet)
lamethyl-1,3-dioxane-4-carbonyl)amide
[No] Propionate structural formula: (R)? Child formula: C36■6■N206 Molecular weight: 642.92 Mass spectrometry calculation value: 642.4607 Actual value 7 64
2.4613 3 7 4 Melting point ("C): oi+ Optical rotation: [α)" -0.4° (C-1.0 C
}lCI! ．． 3) I R (1' naat+
Cm-') :3320, 2932. 2B6
4, 1744. 1654NMR (δ,
CDCj2a): 0.88 (3H, t, J=7Hz)
, 0.90 (3H.s), 1.04 (3H,s
). 1.21-1.38 (20H, m), 1.44
(38, s). 1.47 (3■, S), 1.57-
1.70 (2■, m). 1.92-2.08 (4H
, m). 2.25 (2H, t, J=7Hz), 2
．． 52 (2H, t, J = 6Hz), 3.28 (2H, d
, J=12Hz), 3.46-3.65(2H, m
), 3.69 (IH, d.J=12}1x), 4.
08 (IH, s), 4.29-4.39 (2H, m),
5.29-5.42 (3H, m), 6.60 (IH
, d, J=811z>. 6.93(I}I,t.J
=5Hz), 7.26-7.38 (5H, m) Example 91 Compound name: (S)-2-oleoylamino-2 phenyl
Ethyl 3-(N-(2,2,5.5-tetramethy
-1,3-dioxane-4-carbonyl)amino]1
Oropionate structural formula: (S)? Molecular weight: C38H6■N206 Molecular weight: 642.92 Mass spectrometry calculated value: 642.4607 Actual value: 64
2.4613 Melting point ("C): oN Optical rotation: [α) 2640.2° (C=1.0 CHC
j23) I R (νr+aat+ CIll-
') :3320.2932.2B60,1742.
1660NMR (δ, CDCj2a): 0.
88 (3H, t, J=7Hz), 0.90 (3H.
s), 1.03 (3H, s) 1.21-1.39 (
20 [, m). 1.42 (3Ls), 1.46
(3B, s). 1.57-1.74 (2H, m),
1.92-2.08 (4H, m), 2.25 (2H, t
．． J=7Hz), 2.51(2H,t,J=6[z
) 3.28 (1B, d, J=12Hz), 3.42
-3.67 (2H, m), 3.68 (1■, d, J=1
2Hz), 4.05 (IH, s), 4.31 (IH
, dd, J=12Hz. 5Hz), 4.39(LH
, dd, J=12Hz6Hz), 5.28-5.4
1 (3H, m), 6.59 (10, d, J=8Hz
), 6.91 (IH, t, J=5Hz), 7.25
-7.38 (5H, n+) Example 92 Compound name: (trans) 2 (Oleoid
cyclohebutan-1-yl 3- (N-(
2,2,5.5-tetramethyl-1,3-dioxane-
4-carbonyl)amino]propionate structural formula; (-)-trans-2-aminocyclohe
Molecular formula from ptanol: C3? H66N206 Molecular weight 7 634.94 Mass spectrometry Calculated value: 634.4920 Actual value: 63
4.4911 Melting point (C): oil Optical rotation: [α) 2622.0° (C=1.O CHC
ffi 3) IR(νnest+ CIl1-')'
377 332B. 2932.2864, 1734.1660N
MR (δ, CDC23): 0.88 (3H,
t, J=7Hz). 1.00 (38,s), 1
．． 04(3H,s)1.21-1.38(20f(,m
), 1.41-2.08 (16H, m), 1.43
(3B, s), 1.47 (3H, s), 2.0
9 (2H, t, J = 7Hz) + 2.50 (20 t,
J=6Hz), 3.28(IK,d,J=12Hz
), 3.32-3.44 (IH m), 3.57-
3.68 (IH, m), 3.69 (IH, d.J=12
Hz), 3.99-4.09 (IH, m) 4.08
(LH.s), 4.77-4.84 (IH, n+)
, 5.29-5.40 (2H, m), 5.82 (I
H, d, J=8Hz), 6.97(LH, t, J=
6Hz) Example 93 Compound name: (trans)-2-(oleoyl
amino)cyclohebutan-1-yl 3-(N
- (2,2,5,5-tetramethyl-1,3-diox
trans-4-carbonyl)amino]probionate Structural formula: (+)-trans-2-aminocycloh
From eptanol 3 7 8 Molecular formula: C+J66Nz06 Molecular weight: 634.94 Mass spectrometry calculated value: 634.4920 Actual value: 63
4.49011 Melting point ('C): oil Optical rotation: [α)'' 13.1° (C=1.0 CI
CI! ．． 3) IR (νneat + single mark) 3324, 2932, 2864. 1734. 1
650NMR (δ, CDCjl'+): 0.88
(3B, t, J=7Hz), 0.96 (3H, s),
1.04 (3H, s), 1.21-1.38 (20H
, m), 1.40-2.08 (16H, m), 1.4
3 (3H, s), 1.47 (3H, s), 2.10
(2H, t, J=7Hz). 2.50 (2H, t, J=
6Hz), 3.28(1■, d, J= 12H
z) , 3.51 (2H.dt, J=6Hz, 6Hz)
, 3.69 (IH.d, J=12Hz), 3.97-
4.08 (IH, m). 4.09 (IH, s). 4.
77-4.84 (IH, m). 5.29-5.42 (
2H, m), 5.89 (IH.d, J=8Hz). 6
．． 92 (IH.t, J=6Hz) Example 94 Compound name: (S)-3-methyl-2-oleoylamino
Butyl 3-[N- 2.2.5.5-tetramethyl
-1,3-dioxane-4-carbonyl)amino]pro
Pionate structural formula: Molecular formula: C3sLJzOb Molecular weight: 60B. 91 Mass spectrometry Calculated value 7 608.4764 Actual value 7 60
8.4741 Melting point (C): oil Optical rotation: [α) 244.9° (C・1.O CHCl
3) IR(νnait+Cln-') '3324,
2932. 2860. 1742. 1652NM
R (δ, CDCj2s): 0.88 (3H, t, J=7Hz), 0.93 (3H
．． d, J=6}1z). 0.95 (3H, d, J=6H
z). 0.97 (3H.s), 1.07 (3H.s
), 1.21-1.39 (20H, m). 1.43
(38, s), 1.47 (3H, s), 1.56-
1.86 (3H.s), 1.90-2.08 (4■
+m)+2.20 (2■, t, J=7Hz), 2.
56 (2lI, t, J = 6Hz), 3.28 (IH, d
, J=12Hz). 3.56 (28, dt.J=6F
lz, 611z), 3.68 (LH, d, J=12Hz
). 3.95-4.29 (3H, m), 4.07 (
IH, s), 5.29-5.41 (2H, m), 5
．． 79 (II, d, J = 8Hz), 6.93 (IH
, t, J=6Hz) Example 95 Compound name: (S)-2-oleoylaminobutyl 3-
(N-(2.2,5.5-tetramethyl-1.3 di
Oxane-4-carbonyl)amino]propionate Structural formula: ? Child formula: C34H6■NzOa Molecular weight: 594.88 Mass spectrometry calculated value: 594.4607 Actual value: 59
4.4597 3 8 1 Melting point (C): oil Optical rotation: [α)” 6.2° (C=1.0 CHC
, e 3) IR(νnemt+Cm-') :3
320 2932.2B64.1742.1652N
MR (δ, CDCn3): 0.88 (3H,
t, J = 7Hz), 0.91 (3H, t, J = 7
}1z) 0.97 (3H.s), 1.03 (3H.s)
s), 1.21-1.38 (20H, m), 1.4
2 (3H, s), 1.44-1.68 (4H, m)
, 1.47 (3H, s), 1.91-2.08 (4
Hv), 2.17 (211, t, J=711z)2
．． 58 (2■, t, J=6Hz). 3.29 (1B
, d, J=12Hz), 3.57(2H, dt, J=6
Hz, 6Hz), 3.68 (IH, d, J=12H
z), 4.03-4.24 (3H, m). 4.07
(ILs), 5.29-5.42 (2H, m). 5
．． 84 (LH, d, J = 8Hz), 6.92 (LH,
t, J=6Hz) Example 96 Compound name: 2-oleoylamino-1-phenylethyl
3-(N-(2,2.5.5-tetramethyl1
．． 3-Dioxane-4-carbonyl)amino]propio
Nate structural formula: 3 8 2 ? Child formula: C38H6■N20, molecular weight 7 642.92 Mass spectrometry Calculated value: 642.460? Actual value: 64
2.4606 Melting point ("C): oil Optical rotation: [α) 24'24; 3° (C=1.0
CHCI! ．． 3) I R (VI11111L+
cm-'): 3324, 2932, 2864,
1744. 1660NMR (δ, CDCIs)
: 0.88 (3H, t, J=7Hz), 0.903/2
Fl, s), 0.99 (3/2■, s), 1.03 (
3/2H. s), 1.04 (3/2H, s), 1.1
9-1.38 (20H, m), 1.41 (3/2H,
s), 1.42 (3/2■, s), 1.43 (3H.
s). 1.52-1.66 (2H, m). 1.92-
2.08 (4H, m), 2.12-2.22 (2H,
m), 2.48-2.67 (2H, m), 3.26 (
1/2N, d, J=12Hz), 3.29 (1/2H,
d, J=12Hz), 3.42-3.85 (4H, m
). 3.68 (IH, d, J=12Hz). 4.0
6 (1/2B, s). 4.07 (1/2H, s),
5.29-5.41 (2H, m). 5.84 (1/2H
, d, J=8Hz), 5.86 (1/2H, d, J
=8Hz), 6.16-6.27(IH, m), 6
．． 88-6.97 (LH, m), 7.27-7.38 (
5H, m) Example 97 Compound name: (S)-2-oleoylamino-3-ph
Nylpropyl 3- (N-(2,2,5.5-tetra
Methyl-1,3-dioxane-4-carbonyl)amino
] Propionate structural formula: Molecular formula: C+JaJzOa Molecular weight: 656.95 Mass spectrometry calculated value: 656.4764 Actual value: 65
6.4740 Point ("C): oi1 Optical rotation: [α)" 18.3° (C=1.O CRC
I! ．． 3) IR (νnest+cm-'): 3
316, 2932. 2B60, 1742.
1660NMR (δ, CDCρ3): 0.88 (3H, t, J=7Hz), 0.97 (3
H,s). 1.03 (3H.s), 1.17-1.
38 (20H, m), 1.41 (3H, s).
1.46 (3H, s). 1.50-1.68 (2B, m
), 1.92-2.08 (4B, m). 2.16 (
2H, t, J = 7Hz), 2.59 (2H, t, J
=6Hz), 2. 78 (IH. dd. J=13
Hz. 6Hz) ,2.89(LH.dd.J=13
Hz, 711z). 3.28 (IH, d.J=12
Hz), 3.39-3.69 (2H, m), 3.6
9 (IH, d, J = 12Hz), 4.04-4.09 (
28, m), 4.08 (IH, s). 4.37
-4.47 (LH.m), 5.28-5.41 (2B,
m), 6.07 (1B, d, J=8Hz), 6.9
3 (IH, t, J=5Hz), 7.16-7.32
(58,m) Example 9 Compound name: (S)-4-methyl-2-oleoylamino
Bentyl 3-(N-(2,2,5.5-tetramethane)
Chil-1,3-dioxane-4-carbonyl)amino]
Propionate structural formula: 3 8 5 Molecular formula: C36H66NZO6 Molecular weight: 622.93 Mass spectrometry calculated value: 622.4920 Actual value: 62
2.4895 Melting point ("C): oil Optical rotation: [α) is 7.6° (C=1.O CR
CI! ．． 3) IR(νaait+Clfi-')'
3320, 2932. 2864, 1742. 1
652NMR (δ, CDCl3): 0.88 (3H, t, J=7Hz), 0.91 (3H
,t,J=6Hz),0.93(38,t,J=6Hz
), 0.97 (3■,s), 1.03 (3■+3)
+1.19-1.41 (208 m), 1.42 (3
H, s), 1.47 (3H, s), 1.53-1.7
7 (50, m), 1.90-2.08 (4H, m),
2.17 (2H, t, J=7Hz), 2.57 (2■
+ t+ J・6Hz) +3.28(lH.d, J=
12Hz), 3.56 (2H, dt, J=6Hz, 6
Hz), 3.68 (Ill, d, J=12Hz), 4
．． 07 (LH, s), 3 8 6 4.07 (IH, dd, J=11Hz, 4Hz) +4.
13 (LH, dd, J=11Hz, 4Hz), 4.2
1-4.35 (1■1m), 5.28-5.41 (2H
, m), 5.72 (IH.d, J=8Hz), 6.9
4 (LH. t, J = 6Hz) Example 99 Compound name: 2- (1-oleoylaminocyclohexyl
sil)ethyl 3-(N-(2,2,5.5-tetra
Methyl-1,3-dioxane-4-carponyl)amino
] Propionate structural formula: Molecular formula: Cs-rHbbNtob Molecular weight: 634.94 Mass spectrometry calculated value 7 634.4920 Actual value: 63
4.4899 Melting point (C): oil Optical rotation: (α) 22.0° (C=1.0 C
HCf 3) I R (!' neit+ CT
II-') '3352, 2936. 286
4. 1742. 1664NMR (δ,
CDCns): 0.88 (3tl,t,J=7Hz)
, 0.97(3H,s), 1.04(3H,s
), 1.21-1.67 (32■, m), 1.42
(3H, s), 1.46 (3B, s), 1.91-
2.13 (4H.m), 2.15 (28,t,J=
7Hz) 2.56 (2H t, J=6Hz), 3.
28(II{,d,J=12Hz), 3.46-3.6
3 (2B, m), 3.68 (IH, d, J=12H
z), 4.07 (IH, s), 4.31 (IH, d
, J=11Hz), 4.36 (IH, d, J=11Hz
), 5.13(1}1,s), 5.28-5.42
(2H, n+), 6.96 (II, t, J=5Hz
) Example 100 Compound name: (S)-2-oleoylamino-2-phenyl
Ethyl N-(2.2,5.5-tetramethyl1,
3-dioxane-4-carponyl)aminopropione
Structural formula: Molecular formula: C37■60N206 Molecular weight: 628.90 Mass spectrometry calculated value 7 628.4451 Actual value: 62
8.4440 Melting point ('C): oil Optical rotation: [α) 2946.9° (C=1.O cnc
z a) IR(ν,,eat+ CIll-'): 3
320, 2932, 2864, 1760. 16
62NMR (δ, CDCl3): 0.88 (3H, t, J=7Hz), 1.04 (6H
, s), 1.19-1.38 (2011, m), 1.
43 (3H, s), 1.48 (3H, s). 1.51
-1.69 (2H, m), 1.91-2.05 (41
1, lW), 2.24 (2H.t, J=7Hz). 3
．． 30 (IH.d, J=12Hz), 3.69 (In,
d, J = 12Hz), 3.98 (20, d, J = 5H
z). 4.09 (IH s), 4.39 (IH, dd
, J=11Hz, 6Hz), 4.56 (1B, dd, J
=11Hz. 5Hz), 5.28-5.40(3H,
m) 6.25 (IH, d, J=8Hz). 7.00(
IH, t, J=5Hz), 7.26-7.39 (5H,
m) Example 101 Compound name: (S)-2-oleoylamino-238 9 phenylethyl 4-[N methyl-1.3-dioxamino]butanoate Structural formula: (2,2.5.5-tetra4- Carbonyl) Molecular formula: CsJ6JzO6 Molecular weight: 656.95 Mass spectrometry calculation 4fi: 656.4764 Actual value:
656.4770 Melting point ("C): oil Optical rotation: [α13041.4° (C=1.0 CHC
ffi 3) IR(νR!all CIll-')
:3320. 2932. 2B64. 1744.
1654NMR (δ, CDCfi): 0.88 (38, t, J=7Hz). 0.99 (3H
, s), 1.06 (3H, s), 1.21-1.38
(20Lm), 1.44(3}1,s). 1.48
(3■, S), 3 9 0 1.56-2.07 (8H, m), 2.26 (2H
, t, J=7Hz), 2.32 (2H t.J・6H
z), 3.16-3.38 (2H, m), 3.30
(1■d J=12Hz). 3.70 (IH, d,
J=12Hz), 4.09(LH,s), 4.38
(IH, dd, J=11Hz, 6Hz), 4.44 (1
■, dd. J=11Hz, 5Hz). 5.28-5
．． 42 (38, m). 6.64 (IFI, t, J=5
Hz), 6.76 (IFI, d, J=8Hz), 7
．． 26-7.38 (5H.m) Example 102 Compound name: (S)-2-oleoylamino-2phe
Nylethyl 5-(N-(2.2.5.5-tetramethy
3-dioxane-4-carbonyl)amino pen
Tanoate structural formula: (S) Molecular formula: C4. H66N206 Molecular weight: 670.98 Mass spectrometry calculated value: 670.4920 Actual value: 67
0.4912 Melting point (C): oil Optical rotation: [α)” 40.6° (C・1.0 CI
CI! ．． 3) I R (j' neat+ CI
l1-') :3324. 2932. 286
4. 1742. 1654NMR (δ,
CDCj2s): 0.88 (311, t, J=7Hz
). 0.99 (311, s), 1.05 (3H,
s), 1.20-1.38 (20H, m), 1.4
3 (3H, s), 1.47 (38, s), 1.47
-1.70 (6H, m), 1.92-2.08 (4
H, m), 2.22 (2FI, t, J=7Hz).
2.33 (2H, t, J=6Hz), 3. 12-3
．． 30 (2■, m), 3.29 (10, d, J=1
2Hz). 3.69 (IH, d, J=12Hz),
4.08 (IH, s), 4.28 (IH, dd, J=1
1Hz, 5Hz), 4.43 (IH, dd, J=11H
z. 6Hz), 5.28-5.40 (3H, m). 6
．． 19 (IH, d, J = 8 Hz), 6.68 (In, t
, J=5Hz). 7.26-7.39 (5H, m) real
Example 103 Compound name: (Is,2S)-2-(2,2-dime
hexane-1-yl
3-(N-(2,2,5.5-tetramethyl-
1,3-dioxane-4 monoto structural formula: carbonyl)amino]propione molecular formula: C3llHt. N206 Molecular weight: 650.99 Mass spectrometry calculated value: 650.5233 Actual value: 65
0.5244 Melting point ("C): oil Optical rotation: (α)"10.6' (C=1.0
CHCffiz) IR (ν,,,z, cm-'): 3380, 2932. 2860. 1734NMR
(δ, CDCI!.,) :0.88(3H,t,
J=7Hz), 0.96 (3H, s). 1.04(
3H. s). 1.09 (6H, s), 1.10-2.
16 (38H, m), 1.43 (38, s), 1.4
7 (3B, s). 2.42-2.62 (2H, m),
3.28 (IH, d, J=12Hz), 3.39-3
．． 63 (2H, m), 39 3 /10 3.69 (IH.d, J=12Hz). , 3.81
-3.93 (IH, m), 4.08 (111.s).
4.73 (IH, ddd, J=11Hz, 11Hz
, 4Hz) +5.80 (LH, d, J=8Hz),
6.92 (LH, t, J = 5 Hz) Example 104 Compound name: (Is, 2S) - 2-(2,2-dimethyl
tylooleoyl) aminocyclohexan-1-yl 3
(N-(2,2,5.5-tetramethyl-1,3-dio
Xane-4-carbonyl)amino]probionate Structural formula: Molecular formula: C3sH6eNz06 Molecular weight: 648.97 Mass spectrometry calculated value 7 648.5077 Actual value: 64
8.5063 Melting point (C): oil Optical rotation: [α)” 10.9° (C=1.0 CI
CI! ．． 3) 3 9 4 I R (+'niiat+ cm-'):
3380.2936, 2864, 1734.1672N
MR (δ, CDCj23): 0.88 (3■
, t, J=7Hz), 0.96 (3■, S), 1.
00-2.18 (34H.m). 1.03 (3H, s)
, 1.08 (6■, S), 1.42 (3H.s).
1.47 (3H, s), 2.41-2.62 (2H
, m), 3.28 (IH, d, J=12Hz), 3
．． 38-3.62 (2H, m), 3.69 (IH, d,
J=12Hz), 3.80-3.92 (1■+m)
+4.07 (IH.s). 4.73 (IH, ddd, J
=11Hz, 11Hz, 4Hz), 5.28-5.41
(2H, m), 5.79 (IH, d.J=8Hz)
6.92 (1■, t, J=5HZ) Example 105 Compound name: (Is, 2S) - 2 - (2-method
tylooleoyl) aminocyclohexan-1-yl 3
(N-(2.2,5.5-tetramethyl-1.3-
Dioxane-4-carbonyl)amino]probionate Structural formula: Molecular formula: C3? H66N206 Molecular weight 7 634.94 Mass spectrometry Calculated value: 634.4920 Actual value: 63
4.4950 Melting point C): oil Optical rotation: [α)Z” 10.8° (C=1.0 C
H(4 3)I R (Vnoat+ CI1-')
:3324. 2936. 2864. 1734N
MR (δ, CDCl,)' 0.88 (3H, t, J=7Hz), 0.96 (3B
, s), 1.03 (3H, s), 1.06 (3/2H
, d, J=7Hz). 1.08 (3/2H, d, J=
7Hz), 1.09-2.18 (35H, n+), 1
．． 43 (3H, s), 1.47 (31l, s). 2.
50 (2H, t, J=6Hz), 3.28 (IH, d
, J=12Hz). 3.51 (2H, dt, J=6Hz
, 6Hz), 3.69 (IH, d, J=12Hz)3
．． 81-3.94 (LH, m), 4.08 (IH, s
), 4.61-4.73 (IH, n+), 5.28-
5.42 (2H, m) 5.70-5.78 (10, n+
), 6.91 (IH, t, J=6Hz) Example 10
6 Compound name: (IS.2S) - 2 - (2-method
tyrpalmitoyl) aminocyclohexan-1-yl
3-CN − (2.2.5.5-tetramethyl-1.
3-Dioxane-4-carbonyl)amino]propione
Structural formula: (from upper spot raw material) Molecular formula: C+sFIaJzOb Molecular weight: 608.91 Mass spectrometry calculated value 7 608.4764 Actual value: 60
8.4754 Melting point (“C): 77-79°C (benzene/hexane)
Optical rotation: [α) ” 14.4@(C=1.0 C
HCj23) 397 IR(νKB, , CIl1-'): 3312
, 2932, 2860, 1742. 1
652NMR (δ, CDCffii): 0.
88 (3■, t, J=7Hz), 0.96 (3H,
s). 1.03(3■+S)+1.39(3H,d
, J=7Hz), 1.10-2.18 (35H, m
), 1.43 (3H,s), 1.47 (3H.s)
, 2.43-2.58 (2H.m), 3.28 (I
II, d, J = 12Hz). 3.51 (2H, dt
, J=6Hz. 61Lz), 3.69 (IH, d, J=
12Hz), 3.81-3.93(LH.m), 4
．． 08 (IH, s), 4.68 (IH, ddd, J
=11Hz, 11Hz, 4Hz), 5.76(IH, d
, J=8Hz), 6.91(IH, t.J=6Hz)
) Example 107 Compound name: (Is,2S)-2-(2-method
tyrpalmitoyl) aminohexan-1-yl
3-(N-(2,2,5.5-tetramethyl-1.
3-Dioxane-4-carbonyl)amino]propione
Structural formula: 3 9 8 Molecular formula: Cx5HbaNzOb Molecular weight: 608.91 Mass spectrometry calculated value: 60B. 4764 Actual value 7 60
8.4762 Melting point C): 92-94°C (benzene/hexane)
Luminous intensity: [α)” 6.7° (C=1.0 CFIC
I! ．． 3) IR (νKBr l cm-'): 3
284, 2928. 2860, 1736. 16
52NMR (δ CDC13): 0.88 (3B, t, J = 7Hz), 0.96 (3H
, s). 1.03 (30, s), 1.06 (3H, d
, J=7Hz). 1.10-2.17 (35H, m)
, 1.43 (3H, s). 1.47 (3H, s),
2.50 (2H, t, J = 6tlz), 3.28 (IH
．． d, J=12Hz), 3.5021l, dt, J=
6}Iz. 611z). 3.69 (LH, d, J=12
■z), 3.82-3.95 (IFI, m), 4.0
8 (IH.s). 4.67 (IH, ddd, J=11
Hz, 11Hz, 4Hz) 5.73 (LH, d, J=8
Hz). 6.92 (IH, t, J=6Hz) Example 1
08 Compound name: (IS,2S)-2-(2-ethyl
myristoyl)aminocyclohexan-l-yl 3C
N-(2,2,5.5-tetramethyl-1,3-di
Oxane-4-carponyl)amino]propionate structural formula: (from the upper spot raw material) ? Child formula: C34H6■N206 Molecular weight: 594.88 Mass spectrometry calculated value: 594.4607 Actual value: 59
4.4621 Melting point ("C): oil Optical rotation: [α)" 10.1° (C=1.O CH
Cj23) I R (!' ne+it+ cm-'
) '3320. 2936. 2864.
1734, 1648NMR (δ, CDCj
2s): 0.85 (3H, t, J=7Hz), 0.
88 (3H, t, J=7Hz), 0.96 (3B, s)
．． 1.04 (3H, s), 1.10-2.23
(33H, m), 1.43 (3H, s), 1.47
(3B, s), 2.42-2.59 (2El.m).
3.28 (18, d, J=12Hz), 3.51 (2
H, dt, J = 6Hz + 6Hz) + 3.69 (IH, d
, J=12Hz), 3.82-3.95(IH.m
). 4.08 (IH, s), 4.68 (11, ddd
, J=11Hz, 11Hz, 4Hz), 5.85 (IH
, d, J=8Hz). 6.92 (IH, t, J=6
Hz) Example 109 Compound name: (Is,2S)-2-(2-E
tilmyristoyl) aminohexan-1-yl
3(N-(2,2,5.5-tetramethyl-1.3
-dioxane-4-carbonyl)amino]probione
Structural formula: 40 1 ? Child 2: CIJ6■N206 Molecular weight: 594.8B Mass spectrometry calculated value: 594.4607 Actual value: 59
4.4591 Melting point ("C): Caramel optical rotation: [α)" 9.6° (C・1.0CHCf
3) I R (lKlr l cm-'): 328
8. 2928. 2860. 1736. 1680
．． 1648NMR (δ, CDCj!3): 0.82 (3H, t, J=7Hz). 0.88 (30
, t, J=7Hz), 0.96 (3H, s). 1.0
3 (3H, s), 1.09-2.18 (33H, m)
, 1.43 (38, s), 1.47 (3H, s),
2.41-2.58 (2H, m), 3.28 (IH, d
, J=12Hz), 3.51(2H.dt.J=6H
z, 6Hz), 3.69 (IH, d, J=12Hz),
3.85-3.98(1■+IIIL4.08(IH
, s), 4.68 (IH.ddd, J=11Hz, 1
1Hz, 4Hz), 5.79 (IH, d.J=8Hz)
．． 6.92 (18, t, J=6Hz) Example 110 Compound name: (IS.2S)-2-(2-probi
(rustearoyl)aminocyclohexan-l-yl 3
- ( N - (2,2,5.5-tetramethyl-1
．． 3-Geo402 Xane-4 Oneto Structural formula: carbonyl)amino] Propione (from the upper spot raw material)? Child formula: C39H7■N206 Molecular weight: 665.01 Mass spectrometry calculated value 7 664.5390 Actual value: 66
4.5395 Melting point (c): Caramel Optical rotation: [α)” 9.6° (C=1.O CHC
j! 3) IR (ν78■, cm-'): 328B, 2932. 2860. 1?30. 1
670. 1644NMR (δ, CDCj2, I)
:0.87(3H,t,J=7Hz), 0.88(
3H, t, J=7Hz), 0.96 (3H, s), 1
．． 04 (3H, s). 1.12-2.23 (43H,
m), 1.43 (3}1, s), 1.47 (38, s
). 2.42-2.58 (2H, m). 3.28 (I
I, d, J=12Hz), 3.51 (2H, dt,
J=6Hz, 6Hz), 3.69(LH.d, J=12
1{z), 3.83-3.95 (IH, m), 4.
08(LH,s). 4.68 (LH, ddd, J=
IllHz, 11Hz, 4Hz), 5.82(Ill, d
, J=8Hz), 6.92(IH,t,J=6Hz
) Example 111 Compound name: (IS.2S) -2-(2-p
lobilstearoyl) aminohexan-1-yl
3(N-(2.2,5.5-tetramethyl-1,3-
Dioxane-4-carbonyl)amino]probionate Structural formula: (From lower spot raw material) Molecular formula: C39HffJ206 Molecular weight: 665.01 Mass spectrometry calculated value: 664.5390 Actual value: 66
4.5390 Melting point ("C): 103-105°C (benzene/hexa
) Optical rotation: [α) ” 8.0' (C=1.0
CHCf3)IR(ν Kllr + C
m Ichika), 3288. 2928. 2860.
1730. 1666. 1644NMR (δ,
CDCJ2 3): 0.86 (3H, t.J=7Hz
), 0.88(3H.t.J=7Hz)+0.96(
3H,s). 1.04 (30,s), 1.11-2
．． 21 (43H, m), 1.43 (3H, s), 1.
47 (3H.s), 2.41-2.60 (2H, m)
3.28 (IH.d, J=12Hz), 3.51 (2
H, dt, J = 6Hz. 6Hz), 3.69(IH.d
, J=12Hz), 3.83-3.97(IH, n+
), 4.08 (IH, s), 4.68 (IH.ddd
, J=11Hz, 11Hz+4Hz)+5.77<LH
, d, J=8Hz). 6.92 (ILt, J=6Hz
) Example 112 Compound name: (Is,2S)-2-(1-la
urylcyclobentanecarbonyl) 7 trillion cyclohexane
-1-yl 3-((2,2.5.5-tetrame
Chil-1,3-dioxane-4-carbonyl)amino]
Brobionate structural formula: 4 0 5 Molecular formula: C+J6Jz06 Molecular weight: 620.92 Mass spectrometry calculated value: 620.4764 Actual value: 62
0.4775 Melting point ("C): oil Optical rotation: [α]"9.2" (C=1.0 CH
i3) IR(νnemt+cm-') '3360
．． 2932. 2864. 1732NMR (δ,
CDCI! ．． 3): 0.88 (3H, t, J=7Hz), 0.96 (3■
, s), 1.04 (3H, s), 1.11-2.18
(38H.m). 1.43(31{,s). 1.4
7 (3Ls). 2.42-2.62 (2B, +n),
3.28 (IH, d, J=12Hz), 3.38-3.
42 (28, m), 3.69 (IH, d, J = 12H
z), 3.80-3.92 (IH, m). 4.08
(IH, s). 4.73 (IH.ddd, J=11Hz
, 11Hz. 4Flz), 5.76 (IH, d, J=8
Hz). 6.92 (IH, t, J = 6Hz) 406 Example 113 Compound name: (Is,2S)-2-(1-decyl
cyclobutanecarbonyl)aminocyclohexane-1
3-((2,2.5.5-tetramethyl-1.3 di
Oxane-4-carbonyl)amino]propionate Structural formula: Molecular formula: C33HSBN206 Molecular weight 7 578.84 Mass spectrometry calculated value: 578.4294 Actual value: 57
8.4285 Melting point ('C): oil Optical rotation: [α)22 8J° (c=1.O CHC
l 3) IR (ν,...t, cm-'): 3
336, 2936, 2864. 1734N
MR (δ, CDCffi3): 0.88 (3H, t, J=7Hz), 0.96 (3
H, s), 1.04 (3■.S), 1.06-1.
40 (20H, m), 1.43 (3H, s),
1.47 (3H.s), 1.57-2.34 (12H,
m), 2.43-2.62 (2H, m), 3.28
(1■, d, J=12Hz). 3.41-3.62
(2H, m). 3.69 (IH, d, J=12Hz),
3.81-3.94 (IH, m) 4.07 (IFI
, s), 4.71 (lh, ddd, J=11Hz.
11Hz, 5Hz) 5.59 (IH, d, J = 8tlz
), 7.92 (IH, t, J=5Hz) Example 11
4 Compound name? (Is,2S)-2-(1-olei
(cyclopentanecarbonyl)aminocyclohexane 1
-yl 3-(rl-(2.2,5.5-tetrame
Chil 1,3-dioxane-4-carbonyl)amino]
Ropionate structural formula: ? Child formula: C4■H■N206 Molecular weight: 701.05 Mass spectrometry calculated value 7 702.5546 Actual value: 70
2.5570 Melting point ("C): oil Optical rotation: [α)zz B.6° (C=1.0 CH
C f 3) IR (νR91Ll (J-'): 3368, 2932. 2864. 1734 NMR
(δ, CDCj!s): 0.88 (3H, t, J=7Hz), 0.96 (3H
, s), 1.04 (3H, s), 1.09-2.17
(46H, m), 1.43 (38, s). 1.47
(311.s). 2.41-2.6H2H, m). 3
．． 28 (IH, d, J=12Hz) t3.37-3.6
2 (2H, m), 3.69 (IH, d.J=12Hz
). 3.81-3.93 (18, m), 4.08 (I
H, s) 4.73 (IH, ddd, J=11Hz, 11
Hz, 4Hz), 5.28-5.40 (2H, m).
5.75 (LH, d, J=8Hz). 6.93 (Ill
, t, J=5Hz) Example 115 Compound name: (Is,2S) -2- ((1-methyl
Ru-8-hebutadecenyl)carbamoyl)aminocyclo
Hexan-1-yl 3-(N-(2,2,5.5
-tetramethyl-1,3-dioxane-4-carboni4
0 9 )Amino]propionate structural formula: d+astereomeric mixture molecular formula
: C+JaJlsO6 Molecular weight: 649.96 Mass spectrometry calculated value: 649.5029 Actual value: 64
9.5029 Melting point (C): oil Optical rotation: [α)” 19.3° (C=1.OC
RC I! ．． 3) IR(νflemtH Clfi-'
) :3360, -2936. 2864. 173
4, 1682. 1644NMR (δ, CDC1
3): 0.88 (3H, t, J=7Hz). 0.96 (3H
, s), 1.04 (3H, s). 1.08 (3/21
, d, J=6Hz), 1.09 (3/2H, d.J=
6Hz). 1.144.50 (248, m). 1.4
4 (3H,s), 1.47 (3H.s), 1.52-
2.26 (11B, m). 2.37-2.59 (2F
l, m) 41 0 3.28-3.46 (LH, n+), 3.58-3
．． 80 (3H, n+), 3.69 (1}1, d, J, .
．． 12Hz), 4.10 (IFI,s), 4.55
(IH, ddd, J=11Hz, 11Hz, 4Hz)+
5.28-5.42 (2H, m), 6.86-6.
96(IH,m) Example 116 Compound name: (IS,2S) -1- ((1-methyl
butadecanyl)carbamoyl]aminocyclohexa
N-1-yl 3-[N-1(2.2.5.5-
tetramethyl-1,3-dioxane-4-carponyl)
Amino]propionate structural formula: Molecular formula: CssH6sNa06 Molecular weight: 623.92 Mass spectrometry calculated value: 623.4873 Actual value: 62
3.4852 Melting point (C): oil Optical rotation: [α)” 20.5° (C=1.0 C
HC f 3) IR (!'xir + cm-'
) :3360,2932,2860.1738.1
682.1642NMR (δ, CDCf3)
:0.88 (3H, t, J=7Hz). 0.96(
3■,s), 1.04(3■,S). 1.08 (3
H, d, J=6Hz), 1.12-1.78 (32
H, m), 1.44 (3■.s), 1.47 (3H
．． s), 1. ．． 94-2.58 (4H, m), 3.
28 (IH, d, J=12Hz), 3.34-3.
79 (4H, m), 3.69 (IH, d, J = 12Hz
), 4.10 (IH, s), 4.55 (IH, dd
d, J=11Hz. 11Hz, 4Hz). 6.92 (I
H, t, J=5Hz) Example 117 Compound name: (Is,2S) -2-(1-O
butanecarbonyl)aminocyclohexane
-1-il 3-(N-(2.2,5.5-
Tetramethyl 1,3-dioxane-4-carbonyl)a
Mino] Probionate structural formula: Molecular formula: C3+Hs4Nz06 Molecular weight 7 550.78 Mass spectrometry calculated value: 550.3981 Actual value: 55
0.4005 Melting point (C): oil Optical rotation: [α)” 13.1° (C=1.0 CI
CI ,)IR(ν,,a at + clll −
) :3336. 2932. 2860. 1
732NMR (δ, CDCj!s): 0.88 (3H, t, J=7Hz), 0.96 (3H
, s). 1.04 (3H, s), 1.06-1.58
(16H, m),'. 1.43 (3H, s). 1.
47(3■+S)+1.60-2.36(12H.m)
．． 2.43-2.63 (2H, m), 3.28 (1
8, d, J=12Hz). 3.39-3.63 (2H
, m), 3.69 (IH, d, J=12Hz). 3.
81-3.94 (IH, m). 4.08(IH,s),
4.72 (IH, ddd, J=11Hz, 11Hz,
4Hz), 5.60 (IH, d, J=8Hz), 6.
93 (IH, t, J = 5Hz) 4 1 3 Example 118 Compound name: (Is, 2S) - 2-( 2-isopropylene
lobillauroyl) aminocyclohexan-l-yl 3
-(N-(2.2.5.5-tetramethyl-1,3-di
Oxane-4-carbonyl)amino]propionate Structural formula: (from upper spot raw material) Molecular formula: C33H60N206 Molecular weight: 5B0.85 Mass spectrometry calculated value 7 580.4451 Actual value: 58
0.4435 Melting point ("(:):wax Optical rotation: [α)"11.9' (C=0.9
CHCffi3)IR(JJxi,, CIll-'
) :3288,2932.2860.173041
4 NMR (δ, CDCI!.*): 0.88 (
38, t, J=7Hz). 0.88 (38, d, J
=6■zL0.91 (3H, d, J=6Hz), 0
．． 96 (3H,s), 1.04 (3H.s) 1.0
0-1.82 (26H, m), 1.43 (3H, s
), 1.47 (3H, s), 1.93-2.04 (
III, m), 2.15-2.26 (IH, m),
2.41-2.58 (2H, m), 3.28 (LH
, d, J=12Hz), 3.42-3.60 (211,
m), 3.69 (ill, d, J=12Hz)3.
82-3.94 (IH, m), 4.08 (IH, s
), 4.67 (IH, ddd, J=11Hz, IIH
Z, 4Hz), 5.87 (IH, d, J=8Hz),
6.91 (IH, t, J = 5■2) Example 119 Compound name: (15.25) -2 - (2-iso
(propylauroyl) aminohexan-1-yl
3-(N-(3,3,5.5-tetramethyl-1
．． 3-Dioxane-4-carbonyl)amino]propio
Nate structural formula: Molecular formula: C33H60N206 Molecular weight 7 580.85 Mass spectrometry calculated value: 580.4451
: 580.4458 Melting point ('C): Caramel optical rotation: [α) 3010.6° (C=1.O CHi
3) IR (ν., , cm-'): 3276, 2932, 2860. 1730NMR
(δ, CDCβ,): 0.85 (3H, d, J=6Hz), 0.88 (3H
, t. J=7Hz), 0.89(3H, d, J=61{
z), 0.96 (3H, s). 1.04(3H,s
), 1.05-1.83 (26H, n+), 1.43
(3H, s), 1.47 (3B, s). 1.92-2
．． 04 (IH m), 2.13-2.22 (LH, m
), 2.40-2.58 (211, m), 3.28 (
LH, d, J = 12Hz). 3.45-3.58 (2H
, m), 3.69 (IH, d, J=12Hz), 3.
85-3.97 (IH.m). 4.08 (IH,s)
, 4.68 (1B, ddd. J=11Hz, 11
Hz, 4Hz) ,5.78(IH, d, J=8Hz
), 6.90 (II1, t, J=5Hz) Example 12
0 Compound name: (15.28) − 2 − ( 1-he
xylcyclo4 1 6 butanecarbonyl)aminocyclohexane-1yl 3
- [N-(2,2,5.5-tetramethyl1,3
-dioxane-4-carbonyl)amino]propione
Structural formula: Molecular formula: C29H5. N206 Molecular weight 7 522.73 Mass spectrometry calculated value 7 522.3668 Actual value: 52
2.3668 Melting point (C): oil Optical rotation: [α]” 13.8° (C=1.0 CI
CI23) I R (V IIIIIILI CII
1-') :3336, 2936. 2864.
1732NMR (δ CDCj!+): 0.87 (3H, t, J = 7Hz), 0.96 (3H
, s). 1.04 (3tl,s) 1.07-1.58
(12H, m), 1.42 (3■, s), 1.47
(31{,s)4 1 7 1.61-2.34(128,m). 2.43-2
．． 62 (28, m), 3.28 (IH, d, J = 12H
z). 3.41-3.62 (2H, m). 3.69
(1B, d, J=12Hz), 3.82-3.93
(IH, m) 4.07 (IH, s), 4.71 (IH
．． ddd, J=11Hz, 11Hz, 4Hz), 5.6
0 (IH, d, J=8Hz), 6.92 (IH, t
, J=5Hz) Example 121 Compound name: (Is,2S)-2-(1-butyl
butanecarbonyl) aminocyclohexane-1
3-(N-(2.2,5.5-tetramethyl-1
,3-dioxane-4-carbonyl)amino]propio
Nate structural formula: Molecular formula: C2FH46N206 Molecular weight: 494.67 Mass spectrometry calculated value: 494.3355 Actual value: 49
4.3366 4 1 8 Melting point ("C): Caramel Optical rotation: [α) 3015.2° (C・1.O CHC
13) IR (νKBr + Cm-'): 3348, 2940. 2868. 1732NMR
(δ, CDCJ23): 0.88 (3H, t, J=7Hz). 0.96(3
H,s), 1.04(3H,s). 1.05-1.5
8 (8H, m), 1.43 (3■, s). 1.47
(3H, s), 1.62-2.33 (12H.m).
2.44-2.61 (2H, m), 3.28 (1B, d
, J=12Hz). 3.41-3.63 (2■, m)
, 3.69 (LH, d, J=12Hz), 3.81-
3.94 (18, m). 4.08 (IH, s). 4.
72 (LH.ddd, J=11Hz, 11Hz, 4Hz
), 5.61 (10, d, J=8Hz). 6.
93(In,t,J=511z) Example 122 Compound name: (Is,2S)-2-(1-de
cyclobutanecarponyl)aminocyclohexane
1yl l-[N-(2,4-dihydroxy-3.3di
Methyl-1-oxobutyl)amino]propionate Structural formula: Molecular formula: CsoHsJz06 Molecular weight: 538.7? Mass spectrometry Calculated value: 538.3981 Actual value: 53
8.3989 Melting point (C): oil Optical rotation: [α)” 10.6° (C=1.O CH
CI 3) TR (νneai Cm-'): 2
932. 2860. 1732 NMR (δ, CDCn:+): 0.88 (3H, t, J = 7Hz), 0.97 (3H
, s), 1.05 (3H, s), 1.06-1.44
(20N, m), 1.46-2.28 (12H, m)
, 2.44-2.64 (2B, m), 2.77 (2H
, br-s), 3.46-3.68 (2H, m), 3
．． 49 (LH, d, J = 11Hz), 3.56 (IH,
d, J=lIHz), 3.84-3.98(IH, m
), 4.05 (IH.s). 4.69 (18, ddd
, J=11Hz, 11■214}12) 15.53(I
H, d, J=9Hz), 7.37(IN, t.J=5
Hz) Example 123 Compound name: (Is,2S)-2-(1-methyl
lauroyl) aminocyclohexan-1-yl 31 (
N-(2.2,5.5-tetramethyl-1,3-dio
Xane-4-carponyl)amino]propioneto Structural formula: (From the upper spot raw material) Molecular formula: C31H56N206 Molecular weight 7 552.80 Mass spectrometry Calculated value 7 552.4138 Actual value 7 55
2.4127 Melting point ("C): oil Optical rotation: [α) 3' 15.8° (C=1.0
CICI! ．． 3) I R (vKllr + c
m-'): 3304, 2932, 2860
．． 173842 1 NMR (δ, CDCj23): 0.87 (3
H. t, J=7Hz), 0.95(3H,s),
1.03 (3B, s), 1.07 (3H, d, J=7H
z), 1.10-1.38 (20H, n+), 1.
42 (3H.s). 1.46 (3H.s), 1.4
8-2.19 (7H, m), 2.42-2.57 (2H
, m), 3.28 (IH, d, J=12Hz), 3.
51 (2H.dt, J=6Hz, 6Hz), 3.69
(1■, d, J = 12Hz), 3.81-3.94 (I
H, m). 4.08 (LH, s), 4.68 (IH
, ddd, J=4Hz), 5.76(IH.d, J=
8 Hz), 6.92 (IH, t, J = 6 Hz) Example 124 Compound name: (Is, 2S) -2 - (1-methyl
Lulauroyl) aminohexan-1-yl 3[
N - (2,2,5,5-tetramethyl-1,3-di
Oxane-4-carponyl)amino]probionate Structural formula: (from lower spot raw material) 42 2 Molecular formula: C31HS6NZO6 Molecular weight: 552.80 Mass spectrometry calculated value: 552.413B Actual value: 55
2.4139 Melting point ('C): wa× Optical rotation: [α)'' 7.66 (C=1.0 CH
l3) IR (νκ meter + cm-'): 3272, 2932, 2860. 1744NMR
(δ, CDCI!.3) :0.88(3H,t,
J=7Hz), 0.96(3H,s), 1.03(
3H, s), 1.06 (3H, d, J=7Hz), 1
．． 10-1.39 (20B, m), 1.43 (38, s
), 1.47 (3H.s). 1.49-2.16(
7H, m), 2.50 (2H.t, J=6Hz). 3
．． 28 (1B, d, J = 12Hz), 3.51 (2H,
dt, J=6Hz, 6Hz), 3.69(IH, d,
J=12Hz), 3.82-3.96 (IH.m).
4.08 (IH, m), 4.67 (1■+ ddd+
J=11Hz. 11Hz, 4Hz) +5.73(
IH, d, J = 8Hz). 6.92 (IH, t, J
=6Hz) Example 125 Compound name: (IS,2S)-2-(2-decyl
lauroyl)aminocyclohexan-1-yl 3(
N-(2,2,5.5-tetramethyl-1,3-di
Oxane-4-carbonyl)amino]propionate Structural formula: Molecular formula: 04. H? 4N206 Molecular weight 7 679.04 Mass spectrometry calculated value: 67B. 5546 Actual value: 67
8.5535 Melting point ('C): 70-71°C (hexane) Optical rotation:
[α)” 10.3° (C=1.0 CI{Cj2
,)IR(νKlr + CIll-'): 3288
．． 2928. 2856. 1732NMR (δ,
CDCIl3): 0.88 (6H, t, J=7Hz), 0.96 (3
H,s). 1.04 (3H, s), 1.08-2.2
2 (45H, m), 1.43 (3H, s). 1.4
7 (3H, s), 2.39-2.58 (2H, m),
3.28 (IFI, d, J=12FIz), 3.51
(21, dt, J=6Hz, 6Hz), 3.69(
1■, d, J=12Hz) +3.83-3.96
(LH, m), 4.08 (IH, s), 4.68 (
LH. ddd. J=11Hz, 11Hz, 4Hz), 5
．． 82 (1■, d, J=8Hz), 6.90 (LH
, t, J=8Hz) Example 126 Compound name: (IS.2S) - 2 - (N-deci
RuN-isopropylcarbamoyl)aminocyclohexyl
San-1-yl 3-[ N - (2.2,5.5-
tetramethyl-1,3-dioxane-4-carbonyl)
Amino] propionate structural formula: Molecular formula: C, l! HsqN306 Molecular weight: 581.84 Mass spectrometry calculation value: 581.4403 Actual measurement value:
581.4414 42 5 Melting point ('C): oil Optical rotation: (α)'' 30.1° (C=0.5 CH
Cj2 3) I R (vnesc+ CI1-
'): 2932.2860.1732 NMR (δ, CDCIls): 0.88 (3
H, t, J=7Hz), 0.96 (3H, s),
1.03 (3H, s), 1.10 (6H.d.J=7
Hz), 1.15-2.21 (24H, m). 1.
42 (3H, s), 1.47 (3H, s), 2
．． 47-2.62 (2H, m), 2.93 (2H.t,
J=7Hz). 3.28 (IH, d, J=1211
z). 3.34-3.64 (2H, m). 3.69
(IH, d, J=12Hz), 3.74-3.88 (I
H, n+). 4.08(LH,s), 4.18-4
．． 33 (LH, m). 4.38-4.46 (IH,
m). 4.71 (IH, ddd, J=11Hz, 11H
z, 4Hz), 6.93 (IH, t, J=5Hz)
Example 128 Compound name: (Is,2S)-2-(2-phenylene
aminocyclohexane-1-i
3-(N-(2,2,5.5-tetramethyl-1.
3dioxane-4-carbonyl)amino]propione
4 2 6 Structural formula: (From the upper spot raw material) ? Child formula: CsJs■N206 Molecular weight: 572.79 Mass spectrometry calculation value: 572.3825 Actual value 7 57
2.3841 Melting point C): Caramel optical rotation: [α) ” 5.8' (C=1.O
CHCj23) IR (νKBr + Cm-'):
3304, 2936, 2864, 1734. 1
662. 1646NMR (δ, CDCj2a)
' 0.87 (3■, t, J=7Hz), 0.95 (3H
, s), 1.03 (3H, s). 1.05-1.95
(18H, m), 1.42 (3H, s), 1.46
(38,s), 2.09-2.24(LH.m), 2
．． 37-2.54 (2H.m), 2.68 (28, dd
, J=13Hz, 5Hz). 2.83 (IH, dd, J
=13Hz, 10Hz), 3.28(IH, d, J=1
2Hz), 3.48 (2H, dt, J=6Hz, 6
Hz), 3.68 (IH, d, J=12Hz), 3
．． 70-3.82 (18, m). 4.07 (IH,s)
, 4.50 (IH, ddd, J=11Hz, 11H
z, 4Hz), 5.42 (IH, d, J=8Hz).
6.88 (IH, t, J=6Hz) 7.12-7.2
6(5H,m) Example 129 Compound name: (Is,2S) -2- (2-fe
Nylmethyl(brolyloyl)aminocyclohexane-1-
yl 3-CN-(2,2,5.5-tetramethane)
Chil-1,3dioxane-4-carponyl)amino]
Robionate structural formula: Molecular formula: C3Js2NzO6 Molecular weight: 572.79 Mass spectrometry calculated value: 572.3825 Actual value 7 57
2.3812 Melting point ("C): Caramel optical rotation: [α)"26.1' (C=1.0
CHCIl:+)I R (J'KB+' l cm
-') :3320, 2940. 2B64, 1
734. 1652NMR (δ, CDCI!.3)
:0.87(3■t, J=7Hz), 0.95(3
8,s). 1.03 (3Ls), 1.054.47 (
12H. m), 1.43 (38, s), 1.47 (
3H, s) 1.51-2.31 (9H m). 2.6
1 (IH, dd, J = 14Hz, 5Hz), 2.94 (
IH, dd, J=14Hz, 9Hz), 3.22-3
．． 28 (2H, n+), 3.28 (IH, d, J=12
Hz). 3.69 (IH, d, J=12Hz), 3.
70-3.84 (LH, m), 4.07 (18, s)
, 4.55 (IH, ddd, J=11Hz, 11Hz,
5Hz). 5.93 (LH.d, J=8Hz). 6.
81 (IH, t, J = 5Hz), 7.12-7.30 (
5H,m) Example 130 Compound name: (Is,2S) -2-( 2-phenyl
lauroyl)aminocyclohexan-1-yl 3(N
-(2,2,5,5-tetramethyl-1,3-dioki
San-4-carbonyl)amino]propionate 4 29 Structural formula: Molecular formula: C36HSllN206 Molecular weight: 614.8? Mass spectrometry Calculated value: 614.4294 Actual value 7 61
4.4310 Melting point ("(:):oil Optical rotation: [α] 3° 14.8' (C=0.9 CH
Cj2*)IR(νllemt+CTII-'):
3312 2932, 2860. 1734NMR
(δ, CDCj23): 0.87 (3H.t.J=7Hz). 1.11-1.39 (208, m), 1.52-2.1H61{, m), 3.25 (IH, t, J=7Hz), 3.38-
3.56 (2H, m) 3.77-3.89 (IH, m) 0.97 (3tl, s), 1.05 (3H, s),
1.43 (3H, s), 1.48 (3H, s), 2
．． 32-2.51 (2H, m), 3.29 (IH, d, J=12Hz). 3.70 (IH
, d, J=12Hz), 4.09 (IH, s), 4 3 0 4.59 (LH, ddd, J=11Hz, 11Hz,
4Hz). 5.68 (It{, d.J=8Hz),
6.89 (IH, t.J=5Hz>7.21-7.3
6(5H,m) Example 131 Compound name: (Is,2S)-2-(2-phenylene
lulauroyl) aminocyclohexan-1-yl 3(
N-(2,2,5.5-tetramethyl-1,3-dioxy
San-4-carbonyl)amino]probionate Structural formula: (from lower spot raw material) Molecular formula: (,+aHssNz06 Molecular weight 7 614.87 Mass spectrometry calculated value: 614.4294 Actual value: 61
4.4311 Melting point ("C): wax Optical rotation: [α)" 34.4° (C=1.0 CI
{C 1 3) IR (νKBr + Cm-')
:3308,2932.2864.1730NMR
(δ, coci!3) :0.87(3H,t,J
=7Hz), 0.94 (31Ls), 1.03
(3H, s), 1.09-1.42 (20H.m),
1.43 (3H, s). 1.48(3}1,s)
, 1.52-2.15 (811, m), 3.20-
3.21 (3H.m), 3.28 (IH.d, J=12
Hz), 3.68 (LH.d.J=12Hz), 3
．． 76-3.89 (IH.m), 4.06 (1}1
, s). 4.59 (IH.ddd, J=11Hz. 1
1Hz, 4Hz) 5.75 (IH, d, J=8Hz),
6.71 (1B, t.J=5Hz) 7.19-7.
34 (5fl, m) Example 132 Compound name: (IS.2S) -2-(1-pendi
(cyclopetanecarbonyl)aminocyclohexane-l
yl 3-(N-(2,2,5.5-tetramethyl
-1,3-dioxane-4-carbonyl)amino]pro
Bionate structural formula: Molecular formula: C3. H44NZO6 Molecular weight 7 528.69 Mass spectrometry Calculated value: 528.3199 Actual value 7 52
8.3193 Melting point ("C): caramel optical rotation: [α] 3° 11.9" (C = 1.0 CH
Cj! s) JR (νKlr, cm-'): 33
56. 2944. 2868. 1732NMR (
δ, CDCj! z): 0.84-1.55 (4H, n+), 0.95 (3H
．． s), 1.03 (3H, s), 1.42 (3FI,
s), 1.46 (3Ls), 1.58-2.67 (
12Ln+) 3.00 (1■, d, J=14Hz).
3.03 (IH, d, J = 14Hz), 3.28 (LH
, d, J=12Hz), 3.27-3.52 (2H,
m) 3.68 (IFI, d, J=12Hz), 3.7
2-3.87 (IH, m), 4.06 (IH.s).
4.59 (1■, ddd, J=11Hz, 11H
z+4Hz)+4.51 (IH, d, J=811z),
6.88 (1 ■ r t + J = 5 Hz)
r43 3 7.11-7.28 (5H, n+) Example 133 Compound name: (Is, 2S) - 2 butanetriponyl) 1-yl 3-[N 1,3-dioxampenobionate Structural formula: (l -Furfurylcyclohexane-(2,2,5.5-tetramethyl4-carbonyl)amino] Formula: C28H4■N20, Molecular weight 7 518.65 Mass spectrometry Calculated value: 518.2992 Actual value: 51
8.2969 Melting point ('C): oil Optical rotation: [α) 3012.8° (C=0.5 CHC
n 3) I R (V KBr, cm-
') :3352, 2944. 2868.
17324 3 4 NMR (δ, CDCj2i): 0.96 (3
■,s), 1.03(3}1,s). 1.18
-2.57 (16H, m), 1.42 (3H, s),
1.47 (38,s). 3.03 (2H, s),
3.28 (IH, d, J=12Hz), 3.33-
3.58 (2H, m), 3.69 (IH, d, J=12
Hz), 3.67-3.90 (IH, m), 4.0
7 (LH, s), 4.63 (IH, ddd, J=1
1Hz, 11Hz, 4Hz) 5.49 (IH, d, J=
8Hz), 6.03 (LH.d, J=3Hz), 6
．． 26 (IH dd, J=3Hz, IHz), 6.
92 (IFI, t, J=5Hz) 7.29 (IH, d,
J=IHz) Example 134 Compound name: (Is,2S) -2-(2-penzyl
lauroyl) aminohexan-1-yl 3(N
-(2,2,5,5-tetramethyl-1,3-dioxa
4-carbonyl)amino]propionate Structural formula: (From the upper spot raw material) Molecular formula: C3? H60N206 Molecular weight: 62B. 90 Mass spectrometry Calculated value 7 628.4451 Actual value: 62
8.4442 Melting point ("C): wax Optical rotation: [α) 29-5.9' (C=1.0 C
HCj23)I R (ν,leat+ CIl1-'
) :3320, 2932. 2860. 1732
NMR (δ, CDCI23): 0.62-1.50 (20H, m), 0.88 (3H
, t, J=7}1z). 0.95 (3Ls). 1.0
3 (3H.s). 1.42(3■,S), 1.46(
3H, s), 1.52-2.30 (7H, m) 2.3
8-2.55 (2H, m), 2.68 (IH, dd,
J=15Hz, 6Hz) 2.83(IH, dd, J=1
5Hz, 10FIz), 3.28 (LH, d, J=1
2Hz). 3.48 (2■, dt, J=6Hz, 6Hz
). 3.68 (IH, d, J=12Hz), 3.70
-3.83 (1■, m). 4.07 (IH, s). 4
．． 50 (IH, ddd, J=11Hz, 11Hz
, 5Hz). 5.91 (III, d, J=8Hz)
, 6.88 (IH, t, J=6Hz), 7.11-7
．． 27 (5H.m) Example 135 Compound name: (Is,2S)-2-(2-pe
aminohexan-1-yl
3(N-(2,2.5.5-tetramethyl-1.
3-Dioxane-4-carbonyl)amino]propione
Structural formula: Molecular formula: C3? H6. Nzoi, molecular weight 7 628.90 Mass spectrometry calculated value: 628.4451 actual value: 62
B. 4478 Melting point ("C): I1ax Optical rotation: [α]" 26.7° (C=1.O CH
CI! ．． 3) I R (1'xmr l cm-'
) :3300,2932.2860.1734NM
R (δ. CDC!3): 43 7 0.88 (3H, t, J=7Hz). 0.95 (3H,
s), 1.03 (3H, s), 1.06-1.50 (2
0H, n+). 1.43 (3H, s), 1.4
7 (3H, s) 1.52-2.30 (9H.m),
2.61 (IH, dd, J = 15Hz + 6Hz)
+2.93 (LH, dd, J=15Hz.10Hz).
3.20-3.30 (2}1, m), 3.28 (I
H, d, J = 12Hz), 3.69 (LH, d, J
=12Hz), 3.71-3.83(IH, m),
4.07 (10, s), 4.55 (IH, ddd,
J=11Hz, 11Hz, 4Hz) ,5.91(
IH, d, J = 7Hz), 6.81 (IH, t, J
=5Hz)7.13-7.28(5H,m) Example 136 Compound name: (Is,2S)-2-(1-cinna
milcyclobutanecarbonyl)aminocyclohexane 1
-yl 3-(N-(2,2.5.5-tetramethyl-
1,3-dioxane-4-carponyl)amino]propyl
Onate structural formula: 43 8 Molecular formula: CszHabNzOb Molecular weight: 554.73 Mass spectrometry calculated value 7 554.3355 Actual value 7 55
4.3361 Melting point C): Caramel optical rotation: [α) ” 14.9' (C=1.0
CIICL)IR(νKBr + CII+-'):
3340, 2944, 2868. 1732NMR
(δ, CD(:l3): 0.89-1.57 (4H, m), 0.95 (3H.
s), 1.03 (3H, s), 1.41 (3H, s)
, 1.46 (3 ■, s), 1.58-2.67 (1
2H, m) 2.59 (2H, d, J=7Hz). 3.
27 (ill, d, J=12Hz), 3.32-3.6
3 (2H, m), 3.68 (IH, d, J=12Hz
), 3.82-3.95 (LH, m). 4.06 (I
I, s), 4.68 (LH, ddd, J=11Hz
, 11Hz, 4Hz) ,5.68(IH,d,J
=8Hz), 6.08(IH, dt, J=16Hz,
7Hz) + 6.44 (IH, d, J = 16Hz), 6
．． 88 (IH, t, J=5Hz). 7.17-7.38
(5H, m) Example 137 Compound name: (IS.2S) -2- (1-(3pro
cyclobutanyl] clohexan-1-yl 3-[N tetramethyl-1,3-dioxamponyl]amino]propionate Structural formula: phenynoleaminocy(2,2.5.5 4-cal?) Formula: C3■H411NZO6 Molecular weight 7 556.74 Mass spectrometry calculated value: 556.3512 Actual value: 55
6.3516 Melting point ('C): Caramel optical rotation: [α)'' 12.5° (C=1.0 C}
ICj2. )IR(νxmr + CI!l-')
:3352, 2940. 2868. 17
32NMR (δ, CDCL): 0.95 (38, s), 095-1.56 (6H.m)
, 1.03 (3H, s), 1.42 (3H, s),
1.46 (3H, s), 1.62-2.48 (14
H, n+) 2.51-2.66 (2H, m), 3.
27 (IH, d, J=12Hz), 3.28-3.48
(2H m), 3.68 (IH, d, J=12Hz
), 3.79-3.92 (IH, m), 4.06 (
IH, s) 4.67 (LH, ddd, J=11Hz, 1
1Hz, 4Hz), 5.64 (18, d, J=8Hz)
．． 6.86 (IH, t, J=5Hz), 7.12-
7.30 (5H, m) Example 138 Compound name: (Is,2S)-2-(2.2-diph
phenyllauroyl)aminocyclohexan-1-yl
3(N-(2.2.5.5-tetramethyl-1.3
-dioxane-4-carbonyl)amino]probione
Structural formula: 44 1? Child formula: C4■H6■N206 Molecular weight 7 690.97 Mass spectrometry calculated value: 690.4607 Actual value 7 69
0.4604 Melting point ("C): oil Optical rotation: [α)291B.8"' (C=1.0C
IICL)IR(νnaat+CI-'): 2932, 2860. 1730 NMR (δ, CDCI!.3): 0.87 (3H
．． t, J=7Flz). 0.94 (3H s), 1.
00-1.49 (20H, m), 1.04 (3H, s
), 1.42 (31, s). 1.47 (3H.s).
1.52-2.38 (8H, m), 3.16-3.2
8(1}1,m). 3.28 (IH, d, J=12H
z), 3.36-3.48 (18, m). 3.68(
11, d, J=12Hz). 3.82-3.94 (IH
．． m). 4.07(1}J s) 4.49(LH,
ddd, J=11Hz, 11Hz, 4Hz),
5.52 (1N, d, J=8Hz). 6.82(1}
1, t, J=5Hz), 7.18-7.37 (IOH,
m) Example 139 Compound name: (Is,2S)-2-(2-pe
Hexan-1-yl 3(N-(
2,4-dihydroxy-3,3-dimethyl 1-oxobu
thyl)amino]propionate Structural formula: Molecular formula: C30H411NZO6 Molecular weight: 532.72 Mass spectrometry calculated value: 532.3512 Actual value: 53
2.3524 Melting point ("C): Caramel Optical rotation: [α) 292B.8° (C=1.O CHC
ff. )IR(νnaat+CIll-')'
2936. 2864. 1728 NMR (δ, CDCI!.s): 0.86 (3t
l, t, J=7Hz), 1.06-1.50 (12H,
m), 0.94 (311, s), 1.02 (3H, s) 1
．． 52-2.35 (9Fl, m), 2.64 (IH, dd, J=14Hz, 6Hz), 2.
89 (IH, dd, J=14Hz, 8Hz), 3.
22-3.48 (2■艷), 3.48 (18, d, J=
11Hz), 3.51 (IH, d, J=11Hz)
, 3.72-3.87 (1B, m). 4.03 (1
}1,s),4.54(LH,ddd,J=11l1z
, lIHz, 4Hz), 5.88 (IH, br-s),
7.12-7.29(6H,m) Example 140 Compound name: (Is,2S)-2-(N-benzyl
-Nhexyl(rubamoyl)aminocyclohexane-1
-yl 3-(N-(2,2,5.5-tetramethane)
Chil-1,3-dioxane-4-carponyl)amino]
Probionate structural formula: ? Child formula: C3■H51N306 Molecular weight: 573.78 Mass spectrometry calculation {! : 573.3777 actual measurement
: 573.3752 Melting point ("C) : oil Optical rotation: [α) 2833.2° (C・0.8CHCf
fi3) I R (V naat+ CIl1-')
'3384. 2936, 2864. 1732N
MR (δ, CDCl3): 0.87 (38, t, J=7Hz), 0.96 (38
, s) 0.97-2.18 (16H, m). 1.03
(3H, s). 1.42 (3H, s), 1.46 (3
8, s), 2.32-2.53 (2H, m), 3.1
8 (2H, t, J = 7Hz), 3.26-3.39 (
LH, m), 3.28 (LH, d, J=12Hz),
3.43-3.56 (In, m), 3.69 (IH, d
, J=12Hz), 3.72-3.85(11,n+
), 4.07 (IH.s). 4.36 (IH, d, J
= 17Hz), 4.46 (IH, d.J = 17Hz),
4.50 (IH, d, J = 6Hz), 4.62 (In
, ddd, J=11Hz. 11Hz, 411z
)． 6.88 (IH, t, J=5Hz), 7.1
9-7.37 (5■+m) Example 141 Compound name: (IS.2S) -2-(N-benzyru
N-octylcarbamoyl)aminocyclohexane 4 4
5 ■-yl 3 m (N-(2,2,5.5-te)
tramethyl-13-dioxane-4-carbonyl)amide
] Propionate structural formula: Molecular formula: C34HssNzOb Molecular weight: 601.83 Mass spectrometry calculated value 7 601.4090 Actual value: 60
1.4113 Melting point ("C): oi1 Optical rotation: [α]" 29.7゜IR (1/neat+Cm-')'
(C-0.5 CHC 1 ff) 3368, 2932. 2864. 1732
NMR (δ, CDCffi:+): 0.87
(3H, t, J=7Hz), 0.96 (3B, s)
, 0.97-2.18 (20H, n+). 1.03
(3H.s), 1.42 (3H,s), 4 4 6 1.46 (3■,s), 2.33-2.53 (2F
l, m), 3.18 (2H, t, J=7Hz). 3
．． 26-3.39 (1 ■, III) I3.28 (IH,
m), 3.43-3.56 (IH, m), 3.69
(LH, d, J=12Hz), 3.72-3.85
(IH, m), 4.07 (IH, s), 4.37 (
IH, d, J = 17Hz), 4.48 (IH, d, J =
17Hz), 4.49 (IH, d, J=6Hz).
4.62 (1B, ddd, J=11Hz. 11Hz,
4Hz) + 6.88 (IH, t, J=5Hz),
7.19-7.36 (5H, m) Example 142 Compound name: (is,2S)-2-(N-benzyl
-N-decylcarbamoyl)aminocyclohexane l-i
3-(N-(2,2,5.5-tetrametre
Chil 1,3-dioxane-4-carbonyl)amino]
Ropionate structural formula: Molecular formula 'C3bH5qNsOb Molecular weight: 629.88 Mass spectrometry calculated value 7 629.4403 Actual value: 62
9.438B Melting point (C): oil Optical rotation: [α)” 26.1° (C・1.O CH
Cj21) IR (v71l.1cm-'): 3384, 2932. 2860. 1732NMR
(δ CDCI!.,): 0.88 (3H, t, J=7Hz). 0.96 (3H
, s), 0.79-2.19 (24H, n+). 1.
03 (3H, s), 1.42 (3Ls), 1.46 (
3H, s), 2.32-2.53 (2H, m), 2.
18 (2H, t, J=7Hz), 3.23-3.38
(1}1, m). 3.28 (IH, d.J=12Hz)
．． 3.32-3.55 (IH, m) 3.69 (IH,
d, J=12Hz). 3.70-3.85 (IH.m
), 4.07 (IH.s), 4.36 (IH, d, J
= 17Hz), 4.47 (IH, d, J = 17Hz),
4.48 (IH.d.J=6Hz), 4.61 (L
H, ddd, J=11Hz, 11Hz, 4Hz
)6.89 (IFI, t, J=5Hz), 7.20-
7.39 (5■III1) Example 143 Compound name: (Is,2S)-2-(2-pe
aminocyclohexane-1-y
3-(N-(2,2,5.5-tetramethyl-
1.3-dioxane-4-carbonyl)amino]propyl
Onate structural formula: Molecular formula: C36HSllN206 Molecular weight: 614.87 Mass spectrometry calculated value: 614.4294 Actual value 7 61
4.4295 Melting point (''(:) : wax Optical rotation: [α) 2s 7.76 IR (ν, 1aat+ Cll-') : (C=1
．． O CHCffi3) 3320,2932.2860, l732 NMR (δ, CDCj2+): 44 9 0.62-1.49 (18H, m), 0.88 (3
H, t, J=7Hz). 0.95 (3H, s), 1
．． 03 (3H, s), 1.42 (3B, s), 1.
46 (3H, s), 1.51-1.95 (6H, m
), 2.08-2.19 (IH, m), 2.37-
2.56 (2H, m). 2.68 (IH, dd, J=1
4Hz, 6Hz), 2.83 (IH, dd, J=14H
z, 9Hz), 3.28 (IH, d, J=12Hz
), 3.44-3.52 (2H, m), 3.68 (
IH, d, J = t2Hz). 3.70-3.82 (IH
, n+), 4.07 (LH, s), 4.51 (I
H, ddd, J=11Hz, 11Hz, 4Hz
), 5.42 (IH, d, J=8Hz). 6.8
8 (IH, t, J = 5Hz) 7.11-7.30 (5H
, m) Example 131 Compound name: (Is,2S)-2-(2-pe
aminocyclohexane-1-i
3-[N-(2.2.5.5-tetramethyl
-1,3-dioxane-4-carbonyl)amino]pro
Pionate structural formula: 4 5 0 (from lower spot raw material) Molecular formula: C36HSIN206 Molecular weight: 614.87 Mass spectrometry calculated value 7 614.4294 Actual value: 61
4.4276 Melting point (C): oil Optical rotation: [α)” 27.4° (C=1.0 CH
Cβ3)IR(νnemt, CIll-'): 330
4, 2932. 2860. 1734NMR (δ
, CDCj23): 0.88 (3}1, t, J=7Hz). 0.95(3
H,s). 0.98-1.49 (18H, m), 1.
03 (3H, s), 1.43 (3H, s), 1.47
(3H, s) 1.52-2.30 (9N, m), 2
．． 61 (IH, dd, J=1411z, 6Hz) 2.9
4 (IH, dd, J=14}1z, 91fz), 3.
22-3.29 (2H, +1), 3.28 (LH.d,
J=12Hz), 3.69(1■, d, J=12
FIz) . 3.71-3.84 (IH, m), 4
．． 07 (18, s), 4.55 (IH, ddd, J=1
1Hz, 11Hz, 411z) ,5.91(1}1
, d, J=8Hz), 6.81(IH, t, J=5H
z),7.12-7.28(5H,n+) Example 145 Compound name: (Is,2S)-2-(3-hexy
-2nonenoyl)aminocyclohexan-1-yl3
- [N-(2,2,5.5-tetramethyl-1.
3-Dioxane-4-carbonyl)amino]propione
Structural formula: Molecular formula: C33HSBN206 Molecular weight: 578.93 IR (v lcn+-'): 16601NMR
(δ,): 0.87(3}1,t,J=7Hz), 0.88(
3H. t, J='lHz). 1736 0.96 (38,s). 1.04 (3H, s),
1.10-1.50 (168, m). 1.43 (3H
, s). 1.47 (3H, s), 1.57-1
．． 88 (6H.m). 1.88-2.18 (4H, m)
, 2.43-2.64 (4tl.m). 3.28(
IH, d, J=12Hz), 3.49 (IH, td
．． J=6Hz), 3.69 (IH, d, J=12Hz)
, 3.84-4.02 (IN, m). 4.08 (1
■,s). 4.64 (IH, td, J= flz
). 5.42 (IH, s), 5.67 (IH, d,
J=Hz), 6.92 (IH, m) Example 14
6 Compound name: (IS.2S) -2-(3-F
phenylmethyl 4-phenyl-2-butenoyl) aminocy
Hexan-1-yl 3-(N-(2,
2,5,5-tetramethyl-1,3-dioxane-4-
Carbonyl)amino)propionate Structural formula: Molecular formula '63SH46N206 Molecular weight: 590.83 45 3 Melting point ('C): wax IR (ν, cm): NMR (δ.): 0.93 (3H, s), 1. 00(3B,s),
0.90-2.12 (8H, m), 1.39 (3H.
s). 1.45 (3H.s). 2.24-2.
54 (2H, m), 3.07 (IH, dd, J=H
z, 3Hz). 3.26 (IH, d.J=12Hz
), 3.20-3.64 (2H.m), 3.53 (2H.m), 3.20-3.64 (2H.m), 3.53 (2H.
．． dd, J=15Hz, 5Hz), 3.67 (IH.d
, J=12Hz), 3.80-3.94(IH.m
). 4.04(LH,s). 4.60 (IH, dd
d, J = Hz, 10Hz, 4Hz) 5.76 (IH
, d, J=8Hz), 6.60 (IH, s). 6.84
(IH.t.J=Hz), 7.16-7.42(
IOH,m) Example 147 Compound name: (Is,2S)-2-(3-propylene)
lobil-2nonenoyl)aminocyclohexane-1-y
3-[N-(2,2,5.5-tetramethyl-L
3-Dioxane-4-carbonyl)amino]propione
Structural formula: 45 4 Molecular formula: CzoH5zNzOb Molecular weight 7 536.84 Melting point (:): wax IR (ν, cm-'): NMR (δ
, ): 0.80-0.96 (6H, m), 0.97 (3H,
s), 1.04 (3H, s), 1.06-2.21
(20H.m), 1.43 (3H,s), 1.
47 (3H, s), 2.40-2.67 (4H, m),
3.28 (IH, d, J = 12Hz), 3.49 (
2H, td, J=6Hz, 6Hz), 3.69(LH
, d, J=12Hz), 3.94(LH, ddd, J=
1011z, 8Hz, 4Hz), 4.08(1}1,
s) 4.64 (LH, dcld, J=10Hz.
10Hz. iz)5.42+5.44(1B,s)
, 5.67+5.70 (18, d, J=8Hz)6.
92 (IH, t, J=6Hz) Example 148 Compound name: (15.25) -2-(3-method)
methyl-2-tridecenoyl)aminocyclohexane-1
-yl 3-(N-(2,2i5,5-tetramethyl-
1.3dioxane-4-carbonyl)amino]probio
Nate structural formula: ? Child formula: C3Hs6NgOb Molecular weight: 564.80 NMR (δ, CDCl3): 0.88 (3H
, t, J=6Hz), 0.97(3H,s).
1.04 (3B, s), 1.10-2.21 (26H,
m). 1.43 (38, s). 1.47 (3H
, s). 2.12 (3Ls), 2.50 (2H.t
．． J=5Hz), 3.28(IH, d, J=12Hz)
, 3.41-3.57 (28, m), 3.69 (1
8, d, J=12Hz), 3.86-4. OHL■
+m) 4.09 (IH, s), 4.65 (IH, d
dd, J=10Hz, 10Hz, 4Hz). 5.48 (
IH, d, J = 8 Hz), 6.92 (II, t, J
=5■2) Example 149 Compound name: (Is,2S) - 2 - (2.3-
Dimethyl-2-tridecenoyl)aminocyclohexane
-1yl 3-(N-(2,2,5.5-tetramethyl
-1,3-dioxane-4-carbonyl)amino]pro
Bionate structural formula: Molecular formula: C3JsJzO6 Molecular weight: 578.93 NMR (δ, CDCl3): 0.88 (3H
, t, J=6Hz). 0.96 (3Ls). ].
．． 03 (3H, s). 1.07-2.21 (26FI.
m), ]. ．． 43 (3LsL 1.46 (3H.
s). 1.63 (311, s), 1.75 (3H,
s), 2.53 (2H, t.J=6Hz), 3.28
(IH, d, J=12Hz), 3. -3.64
(211, n+), 3.69 (IH, d, J=12Hz
), 3.88-4.04 (IH, +n), 4.08
(IFI,s), 4.68(LH,ddd.J=10
Hz, 10Hz, 4Hz), 5.23+5.58(11
1. d. J=9Hz), 6.92(IH,t,J=
5■2)457 Example 150 Compound name: (Is, 2S) - 2 - (to 3-
xylnonanoyl)aminocyclohexan-1-yl
3(N-(2,2,5.5-tetramethyl-1,3
-dioxane-4-carbonyl)amino]propione
Structural formula: Molecular formula: C33L. N206 Molecular weight: 580.95 NMR (6, CDCj23): 0.87 (6
11, t. J=6Hz). 0.96 (3H, s),
1.04 (311, s) 1.10-2.20 (31
H, m), 1.43 (311, s), 1.4"
/(3B,s)2.50(2H,t,J=6Hz).
3.28 (IH, d, J=12Hz). 3.36-3.
60 (2H, m). 3.69 (IFI, d, J=1
2Hz), 3.88 (LH, m), 4.09 (IH
,s),4.64(11{,ddd,J=I.OIIz
．． ]011z. 4Hz), 5.88 (IH, d, J=8
Hz), 6.9]. (].H, t, J=611z)
4 5 8 Example 151 Compound name: (Is,2S) 2-dodecenoyl monoyl 3-[N 1,3-dioxaneprobionate Structural formula: 2-((E)-3-phenylaminosichexane-1 (2,2,5.5-tetramethyl=4-carbonyl)amino] Molecular formula: Cs6H5Jz06 Molecular weight 7 612.94 NMR (δ, CDCn3): 0.55-0.73 (IH.m), 0.97 ( 3H,t
, J=6Hz), 0.96 (3H, s), 1.04
(3H, s). 1.08-2.84 (21■+II
l) +1.42 (3Ls). 1.47 (3H.s)
．． 2.30-2.43 (2}1, m). 2.48 (
2H,t,J=6Hz), 3.28(IH.d,J
=12Hz), 3.33-3.62 (2H.m).
3.69 (IH.d, J=12Hz), 3.70-3.
86 (10, m), 4.08 (LH, s), 4.2
8 (1■, ddd, J=10Hz, 10Hz+
4FIz) 5.06 (IH, d, J=9Hz). 5
．． 85 (LH, s) 6.92 (LH, t, J=6Hz)
, 7.12-7.43 (5H, m) Example 152 Compound name: (Is,2S) 2-dodecenoyl) monoyl 3-[N 1.3-dioxaneprobionate Structural formula: 21(Z)-3 -phenylaminocyclohexane-l (2. 2. 5. 5-tetramethyl 4-carponyl
) Amino] Molecular formula: C36BS6N206 Molecular weight: 612.94 NMR (δ, CDCfi 3): 0.86 (
3H, t. J=7Hz), 0.90(3H.s),
0.99(3■+S)+1.03-2.28(22
Lm). 1.39(3}1,s). 1.44 (
3H. s), 2. 40-2.6 (2■, m),
2.90-3.20 (20, m), 3.25 (IH, d
, J=12Hz), 3.36-3.63(28, m
), 3.66 (IH, d, J=12Hz). 3.9
1-4.02 (1■1111) 14.06 (IH, s)
, 4.65 (IH, ddd, J=10Hz.10H
z, 4Hz), 5.82 (LH, s), 6.04 (
1■, dl J=8! lz) 16.91 (IH, t
, J=6Hz). 7.29-7.44 (5H, m)
Example 153 Compound name: (IS.2S) - 2 - ( (Z)
- 3-7ale 2-nonenoyl]aminocyclohexyl
San-1-yl 3-(N-(2,2.5.5-
tetramethyl-1,3-dioxane-4-carbonyl)
Amino]probionate structural formula: Molecular formula: CsJsoNzOa Molecular weight: 570.85 46 1 NMR (δ, CDCN3): 0.83 (3H
, t, J=7Hz), 0.90(3}1,s),
0.99 (3H, s), 1.08-2.60 (18H
, m), 1.39 (3H, s), 1.44 (3
H, s), 2.94-3.20 (2H, m), 3.
25 (IN, d, J=12Hz). 3.38-3.61
(2H, m), 3.66 (1B, d, J=12Hz
). 3.90-4.04 (IH, m), 4.06 (
1■+5)+4.65(IH, ddd, J=11Hz,
11Hz, 4Hz), 5.82 (IH.s). 6.
0HIH, d, J=6Hz), 6.91(IH, t
, J=611z), 7.29-7.44 (5H, +w) Example 154 Compound name: (Is, 2S) - 2 - ( (E)
- 3-phenyl-2-nonenoyl]aminocyclohex
Sun-1-yl 3-(N-(2,2,5.
5-tetramethyl-1,3-dioxane-4-carboni
) Amino] propionate Structural formula: 46 2 Molecular formula: CzJ15oNzOb Molecular weight: 570.85 NMR (δ, CDCl3): 0.55-0.
72 (IH.m), 0.85 (3H, t.J=7
Hz), 0.96 (3H, s), 1.04 (3H,
s). 0.88-1.99 (15H.m). 1.4
2 (3H, s), 1.47 (314, sL 2.
29-2.34 (2H, m). 2.48 (2H, t, J
=6Hz>. 3.28 (IH, d.J=12Hz)
, 3.32-3.61 (2H.m). 3.69 (I
H, d, J=12Hz), 3.71-3.84 (LH,
m), 4.08 (IH, s), 4.28 (10, d
dd, J=10Hz, 10Hz, 4Hz), 5.07(
1■, d, J=9Hz), 5.85 (IH, s),
6.92 (10, t, J=6Hz). 7.13-
7.45 (5H, m) Example 155 Compound name: (IS,2S) -2 - (2-hex
cylideneoctanoyl) aminocyclylhexane-1-y
3-(N-(2,2,5.5-tetramethyl-1,3
-dioxane-4-carbonyl)amino]probione
Structural formula: Molecular formula: CsJsJzO6 Molecular weight: 564.90 NMR (δ, CDCI!.3): 0.87 (
3H. t, J=8Hz). 0.88 (3H, t, J
=7Hz)0.96(3H,s), 1.03(31
{,s), 1.07-2.26(26H,m), 1
．． 42 (311, s). 1.46 (3H.s),
2.40-2.66 (2H.m). 3.28 (IH, d
, J=12Hz). 3.37-3.64 (2H, m)
．． 3.69 (IH, d, J=12Hz). 3.90
-4.06 (IH, m), 4.07 (LH, s). 4
．． 70 (LH, ddd, J=10Hz, 1011z.4
Hz), 5.38 (IH, t, J=7Hz). 5.
61 (IH, d, J=8Hz), 6.91 (LH,
t+ J=6Hz) Example 156 Compound name: (Is,2S)-2-(2-he
xylideneoctanoyl)aminocyclohexane-1-
yl3-(N-(2.2.5.5-tetramethyl-
1,3-dioxane-4-carbonyl)amino]propyl
Onate structural formula: ? Child formula 203■H86Nl! 06 Molecular weight: 564.90 NMR (δ, CDCfs): 0.88 (38
, t, J=71Lz), 0.89(3H, t, J=
7Hz). 0.96 (31, s), 1.03 (38
, s), 1.06-2.33 (268, m). 1.
42 (3H, s), 1.47 (38, s). 2
．． 40-2.60 (2■, m), 3.28 (LH, d.
J=12Hz), 3.32-3.62(2■+II
L3.69 (18, d, J=12Hz), 3.86
-4.02 (11, m). 4.07 (IH, s),
4.74 (IH, ddd.J=11Hz, lIHz.4
Hz). 5.82 (1■, d, J=8Hz). 6.
01 (18, t, J=7Hz), 6.90 (IH,
t, J=6Hz) Example 157 Compound name: (Is,2S)-2-(N-benzyl-N
nonylcarbamoyl)aminocyclohexane 46 5 1-yl 3-[N-(2,2.5.5-te
tramethyl 1,3-dioxane-4-carbonyl)amide
[No] Probionate structural formula: Molecular formula: C3sH5rNzOh Molecular weight: 615.86 Melting point ("C): oil NMR (δ, CDCf3): 0.88 (3H
, t, J=7Hz). 0.96 (3H.s), 1.
03 (3H, s). 1.05-2.23 (22H, m)
, 1.42 (3H, s). 1.46(3H,s
), 2.32-2.53 (2H, m), 3.17 (
2H, t. J=7Hz) 3.25-3.39(IH, m
), 3.28 (IH, d, J=12Hz), 3.4
2-3.55 (IH, +n), 3.68 (IH, d
, J=12Hz), 3.71-3.83(IH, m),
4.07 (IH, s), 4.36 (IH, d, J=
16Hz), 4.46 (IH, d, J=16Hz)
, 4.47 (IH.d, J=8Hz). 46 6 4.62 (IH, ddd, J=1111z, 11Hz.
4Hz), 4.87 (LH, t, J=6Hz), 7.
20-7.37(58,m) Example 158 Compound name: (Is,2S)-2-(2-pendi
(undecanoyl) aminohexan-1-yl N
- (2,2,5,5-tetramethyl-1,3-dio
Xane-4-carbonyl)aminoacetate Structural formula: Molecular formula: CssHsaNzOb Molecular weight: 600.84 Melting point ("C): oil NMR (δ, CDCI!.3): 0.88 (
3H,t,J=7Hz), 1.02(3H,s),
1.08(3■+S)+1.12-2.24(25
H, s+). 1.46 (3H, s). 1.54
(3Fl.s). 2.61 (IH, dd, J=13Hz
, 5Hz). 2.92 (IH, dd, J=13Hz, 9
Hz), 3.22 (IH, dd, J=18Hz, 5Hz
), 3.31 (IH, d, J=12Hz), 3.70-
3.84 (IH, m), 3.71 (IH.d, J=
12Hz), 3.94 (IH.dd, J=18Hz, 7
Hz). 4.13 (LH, s) 4.62 (Hl.
ddd, J=11H2, IIHZ, 4HZ),
5.51 (IH, d, J=8Hz), 6.64-6
．． 72 (IH, m). 7.14-7.21(3}!,m
), 7.23-7.32 (2}1, m) Example 15
9 Compound name: (IS.2S) - 2 - (2-he
butylnonanoyl)aminocyclohexane-l-yl
3(N-(2,2,5.5-tetramethyl-1,
3-dioxane-4-carbonyl)amino]probione
Structure formula: ? Child formula: C34H6■N206 Molecular weight: 594.88 Melting point (℃): Shunaκ NMR (δ, CDCI23): 0.87 (6
H, t, J=7Hz), 0.96 (3H, s), 1.0
4 (3H.s), 1.08-2.21 (331, m),
1.43 (3H, s). 1.47 (3H, s)
．． 2.41-2.58 (2H, m), 3.28 (I
H. d, J=12Hz), 3.51(28, dt.J=
6Hz. 6Hz). 3.69 (1■, d, J=1
2Hz) 13.82-3.95 (IH, m), 4
．． 08 (IH.s). 4.68 (1B, ddd, J=1
1Hz. 11Hz. 4Hz). 5.80 (11, d, J
= 8Hz), 6.91 (IH, t, J = 6Hz) Actual
Example 160 Compound name: (Is,2S) -2- ((1-hep)
tyloctyl)carbamoyl)aminocyclohexane 1
-yl 3-(N-(2.2.5.5-tet)
lamethyl-1,3-dioxane-4-carbonyl)amide
] Propionate Structural formula: 46 9 Molecular formula: 034H63N306 Molecular weight: 609.89 Melting point (℃): Ax NMR (δ, CDCf!3): 0.87 (6
H, t, J=7Hz), 0.96 (3H, s),
1.03 (38, s), 1.08-2.28 (32H
, m), 1.44 (3H.s), 1.47 (3
H,s). 2.38-2.57 (2B, +n). 3.
28 (IH, d, J=12Hz), 3.31-3.42
(IH, n+), 3.54-3.82 (311, m
). 3.69 (10, d, J=12Hz), 4.1
0(IH,s). 4.48 (LH, br-s), 4
．． 55 (In, ddd, J=11Hz.11Hz, 4H
z). 4.83 (IH, br-s). 6.90 (11
, t, J=6Hz) Example 161 Compound name: (IS, 2S) - 2 - (2-be
3-phenylprobanoyl)aminocyclohexa
N-1-yl 3-(N-(2.2.5.5
-tetramethyl-1,3-dioxane-4-carbonyl
) Amino]probionate Structural formula: 47 0 Molecular formula: C34H46N206 Molecular weight: 578.75 Melting point ("C): Caramel NMR (δ, CDCffi3): 0.94 (3H
．． s). 0.95-2.23 (IH, n+), 1.
03 (3■, S), 1.42 (3H, s), 1.46
(3B, s), 2.43-2.56 (IH.m). 2
．． 68-3.09 (4H, m), 3.15-3.32
(2H, m), 3.27 (2B, d, J=12Hz).
3.59-3.69 (IH, m), 3.68 (1■,
d, J=12Hz), 4.06 (IH.s). 4.3
5 (IH, ddd, J=11Hz, 11Hz.
4Hz). 5.38 (IH, cl, J=8Hz),
6.77 (IH, t, J=6Hz), 7.12-7.
28 (IOH, m) Example 162 Compound name: (Is, 2S) -2 - (4-fe
Nyl-2(3-phenylprobyl)pentanoyl)ami
Hexan-1-yl 3-(N-(2,2
,5,5-tetramethyl-II3-dioxane-4cal
[bonyl)amine]probionate Structural formula: Molecular formula: CssHsaNzOb Molecular weight: 634.86 Melting point (°C): Caramel NMR (δ. CDCI!.3): 0.93 (31, s), 0.98-2.27 ( 198
, m), 1.02 (3H, s), 1.41 (3H, s
), 1.46 (3H, s). 2.48-2.64(
4H, m). 3.12-3.28 (2H, m), 3.
27 (1■, d+ J=12Hz) 13.67 (1
■, d, J=12Hz). 3.78-3.91 (IH
, n+), 4.05 (IH, s). 4.59 (18,
ddd, J=11Hz, lIFlz, 4Hz), 5.8
7 (IH.d, J=8■z), 6.75 (IH,t,
J=6Hz), 7.11-7.30 (10Hv+) Example 163 Compound name: (15.2S) -2-[5-phenyl
-2(4-phenylpuchubiru)pentile]aminosic
Hexan-1-yl 3-(N-(2,2
, 5,5-tetramethyl-1,3-dioxane-4-ka
[rubonyl)amino]probionate Structural formula: Molecular formula: C4. HssNzOb Molecular weight: 662.91 Melting point ("(:): oil NMR (δ, CD(f!a): 0.84-2
．． 14 (21■.m). 0.94(31{,s),
1.01 (3H, s). 1.41 (38, s). 1.
45 (3H.s). 2.32-2.61 (6H, m)
, 3.27 (IH, d, J=8Hz). 3.37-
3.53 (2FI, m), 3.67 (IH.d.J=8
Hz), 3.78-3.92 (IH, m). 4.06
(LH.s), 4.62 (LH.ddd, J=11H
z. 11Hz, 4Hz), 5.82 (LH, d, J=8
Hz). 6.86 (IH, t, J=6Hz), 7.1
1-7.29(IOH,m) 4 73 Example 164 Compound name: (IS.2S)-2 thylbenzyl)-3-nyl)propanoyl] 1-yl 3-[N II3-dioxanebutionate Structural formula: (2 (p-tert-bu(4-tert-butylpheaminocyclohexane(2,2,5.5-tetramethyl4-carbonyl)amino) Formula: C4■H6■N206 Molecular weight: 690.97 Melting point ( "C): Caramel NMR (δ, CDCI!.3): 0.94 (3H
,s), 1.02(3H.s), 1.05-1.8
4 (8B, m), 1.28 (9Fl, s), 1.29
(98,s), 1.4H3■+s) 1.46(3H,
s), 2.12-2.34 (2H, m) 2.48-2
．． 58 (IH.m). 2.66-3.04 (4H, m
), 474

Claims (1)

[Claims] General formula ▲ Numerical formulas, chemical formulas, tables, etc. ▼ (I) In the formula, R^1 and R^2 are the same or different and each represents a hydrogen atom or a protecting group for a hydroxyl group; R^ 3 is a C_5 to C_2_5 monovalent aliphatic hydrocarbon group or group that is saturated or unsaturated and may be substituted with a linear, branched, or cyclic aromatic group ▲ There are mathematical formulas, chemical formulas, tables, etc. ▼ Here, R^4 represents a saturated or unsaturated linear, branched or cyclic C_5 to C_2_5 monovalent aliphatic hydrocarbon group, and R^5 is a hydrogen atom or a saturated or unsaturated Represents a monovalent aliphatic hydrocarbon group which is saturated and optionally substituted with a linear, branched or cyclic aromatic group; A is saturated or unsaturated and linear, branched or cyclic C_2 which may be substituted with an aromatic group of
~C_1_6 represents a divalent aliphatic hydrocarbon group, a divalent aromatic hydrocarbon group, or a divalent aromatic heterocyclic group; Either one of X and Y represents ▲There is a numerical formula, chemical formula, table, etc.▼, and The other is -O-, -S- or ▲ formula,
There are chemical formulas, tables, etc. A compound represented by ▼, where R^6 and R^7 each represent a hydrogen atom or a lower alkyl group; n is an integer from 1 to 4.