TW304860B - - Google Patents

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TW304860B
TW304860B TW83111584A TW83111584A TW304860B TW 304860 B TW304860 B TW 304860B TW 83111584 A TW83111584 A TW 83111584A TW 83111584 A TW83111584 A TW 83111584A TW 304860 B TW304860 B TW 304860B
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formula
alkyl
phenyl
compound
substituted
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TW83111584A
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Chinese (zh)
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Ciba Geigy Ag
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Description

五、發明説明(/ A7 B7 本發明像闋於一種新穎的殺II活性式I化合物 C3 ΗV. Description of the invention (/ A7 B7 The present invention resembles a novel compound of formula I with killing II activity C3 Η

A R3 物 1 合 R 混 &lt; 物 Ν 構 或 · 異和 1 丨 其子 1 和丨 ,原 R H R 物氮 ο C ο 構為為為為 異 X γ ΧΥ 其 } ) 及 a b 中 其 2A R3 compound 1 and R mixed <Ν configuration or · Xiehe 1 丨 its son 1 and 丨, the original R H R compound nitrogen ο C ο is configured to be hetero X γ ΧΥ its}) and a b of 2

R 或 —I- n— ^^^^1 nn ^1.^1 ^^^^1 ^^1 (請先閲讀背面之注意事項再填寫本頁) 中 其R or —I- n— ^^^^ 1 nn ^ 1. ^ 1 ^^^^ 1 ^^ 1 (please read the precautions on the back before filling in this page)

R 為R is

CC

、1T R 和, 1T R and

基 4 R N 或 ί 子 , 原氫 CSI 氣為 1 為 1 R A RBased on 4 R N or 子, the original hydrogen CSI gas is 1 is 1 R A R

C C /|\ ; 或 基氫 烷為 } 立 4 獼 C 白 I 0C C / | \; or the base hydrogen is} Li 4 K C white I 0

基 烷 \1/ 4 CAlkyl \ 1/4 C

基 糲 基 丙 琛 基 烷 \«/ 4 C 經濟部中央標準局員工消費合作社印製 基Base 粝 基 Prosperyl base Alkyl \ «/ 4 C Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

氫 為 2 RHydrogen to 2 R

CC

DD

C CC C

烷 琢 \—/ 6 CAlkane \ — / 6 C

C 線 素 鹵 為 其 f 者 同 不 或 同 相 ; 為 基基 吩 D 讜 或C-line plain halogen is the same or not in the same phase as f; it is the base phen D or

烷 4 C I 1 C 本紙張尺度適用中國國家標準(CNS ) Μ規格(210X297公釐) 五、發明説明(工) A7 B7 經濟部中央標準局員工消費合作社印製 基 9 ( C 1 一 C 4 ) 院 氣 基 9 ( C 1 — C Z ) 豳 烷 基 9 ( C 1 — C Z ) 鹵 烷 氣 基 » ( C 3 — C 6 ) 烯 氣 基 参 ( C 3 — C 6 ) 炔 氣 基 • ( C 1 — C 4 ) 次 院 基 二 氣 基 » 氡 基 或 硝 基 1 η 為 0 * 1 2 $ 3 或 4 * Ζ 為 — 0 — • — 0 一 ( C 1 — C 4 ) 院 基 — » — ( C 1 — C 4 ) 烷 基 一 0 一 9 — S ( 0 ) - (C ! -C 4 ) 烷 基 — S ( 〇 ) - ~ 9 -S (Ο ) S — ( C 1 — C 4 ) 烷 基 — » m 為 0 • 1 9 或 2 t B 為 ( C 1 — C 6 ) 院 基 • 鹵 一 ( C 1 一 C 6 ) 院 基 9 ( C 3 — C 6 ) 琿 院 基 • 或 為 ( C Z — C 6 ) 烯 基 或 ( C 2 — C 4 ) 炔 基 — ( C 1 — C 2 ) 烷 基 » 毎 傾 未 被 取 代 或 被 1 到 3 櫥 鹵 原 子 取 代 , 或 為 芳 基 或 雜 琛 基 其 m 白 獨 立 地 未 被 取 代 或 被 ( C 1 — C 6 ) 烷 基 » 鹵 素 — ( C — C 6 ) 烷 基 &gt; 鹵 素 » ( C 1 — C 6 ) 院 « 基 或 鹵 素 — ( C 1 — C 6 ) 院 氧 基 單 取 代 到 五 取 代 • 或 為 R5 .r7 — (CH)-A &lt;1 Λ 、r8 或 三 甲 基 甲 矽 烷 基 » R 5 $ R 6 $ R 7 9 R 8 和 R 9 値 白 m 立 為 氫 $ ( c — C 4 ) 院 基 或 鹵 素 $ 和 P 為 0 9 1 9 2 或 3 1 -8- — ^------A I裝------訂-----ί 線 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS )八4規格(210Χ297公釐) 經濟部中央標準局員工消費合作社印製 A7 ______B7_ 五、發明説明(j ) R3為氫,(Ci _C6 )烷基,含1到5個鹵原子 的(C, -ce )鹵烷基,(Ci -C4 )烷氣基一(Ci —C2 )院基,(Cz — C* )嫌基一(Ci —C2 )院 基,其像未被取代或被1到3镳曲原子取代,(C2 — C4 )炔基一 (Ci _C2 )烷基,未被取代或被1到4 宿鹵原子取代的(C3 _Ce )琛烷基,未被取代或被1 到4値鹵原子取代的(C3 — C6 )琛烷基一 (Ci -C4 ) 院基,氣基一 (Cl —C4 )焼基;(Cl —C4 )烧氣 基羰基一 (Ci 一(:2 )烷基,(Ci -c4 )烷氣基氨 基甲睡—(Cl — C2 )焼基》苯基一 (Ci — C3 )院 基•其像未被取代或被鹵素,(Cl 一c3)烷基, (Ci _C4 )烷氣基,(Ci -c4 )鹵烷基,氱基, 硝基或(Ci _C4 )次烷基二氣基取代,其苯基裨相同 或不同取代基單取代到三取代;未被取代的苯基或被個自 獼立被(C! -C4 )烷基,(Ci -C4 )烷氣基,齒 素,含1到3倕鹵素原子的(Ci —C2 )鹵烷基,硝基 或«基單取代或二取代的苯基,或未被取代的吡啶基或被 値自獨立被(Ci _C4 )烷基,(Ci _C4 )烷氧基 ,鹵素,含1到3傾曲素原子的(Ci 一〇2 )豳烷基, 硝基或《基單取代或二取代的吡啶基; R4為(Ci —C4 )烷基,苯基,或 R3和R4 —起舆其所鍵结的氮原子形成飽和或不飽 和之5到7員琢,該琛未被取代或被(Ci _C4 )烷基 本紙張尺度適用中國國家橾準(CNS ) Α4規格(210X297公釐) ------Μ 1裝------訂-----(線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央橾準局員工消費合作社印裝 A7 B7 五、發明説明(&gt; ) 取代基取代,可含1到3雇額外的灌自氣,氣和硫之雜原 子。 本發明的化合物具備殺徽豳,殺恙龕和殺昆蠹特性. 適合作為農業、圃蕕和術生學領域的活性成份。 本發明進一步亦鬭於一種製備本發明化合物的方法, 以及鼸於殺徽菌,殺恙蠱和殺昆典組成物,該组成物僳含 此化合物作為活性成份,以及两於此化合物和組成物在控 制植物致病(Phytopathogenic)徽菌,恙巖和昆龕以及預防 受到此種攻擊。 如果式I化合物含非對稱磺原子,此化合物就以光學 活性形式存在。此化合物在任何情況下以〔E〕和/或〔 Z〕形式存在,只是因為有脂肪条,草醯胺和胼叉 (hydrazono) 雙鍵。再者,也可能存在阿托異構活性 (atropisoieris·)。式I欲包括所有逭些可能的異構形式 和其混合物,例如消旋混合物和任何〔E/Z〕混合物。 除非特別定義,上文和下文所用的名詞的定義如下: 鹵素為氟,氛,溴或碘,待別是氟,氯或溴,更待別 是氟或氣。 烷基為直鏈,例如甲基,乙基,正丙基,正丁基,正 己基,正辛基,正癸基,正十二基,正十六基或正十八基 ,或支鏈,例如異丙基,異丁基,二级丁基,三级丁基, 異戊基,新戊基或異己基。 烯基為直鏈或支鰱烯基,例如乙烯基,1_甲基乙烯 -10- 本紙張尺度適用中國國家標準(CNS ) A4規格(2丨0X297公釐) I:------Jkl 裝------訂-----(線 (請先閲讀背面之注意事項再填寫本頁) 304860 _^___ 五、發明説明(灰) 基,烯丙基,ι_丁烯基,異丙烯基,特別是嫌丙基。 炔基例如為乙炔基,1一丙炔基或1一丁炔基•特別 是丙炔基。 應該理解環烷基為琢丙基,琢丁基,琛戊基或嫌己基 〇 ϋ素取代基例如鹵烷基和鹵烷氣基可部份或完全被相 同或不同取化基豳化。鹵烷基的實例為被氣,氨和/或 澳單取代到三取化的甲基,例如CHF2 , CFs或CHCU ;被 氟,氨和/或溴單取代到五取代的乙基•例如Cli2 CF3 ’ CF2 CF3 . CF2 CCI3 , CF2 CHC12 , CF2 CCI3 , CF2 CHC1 2 . CF 2 CHF e , CF z CFClz , CH2 CHz Cl, CFz CHBr2 · CFz CHC1F, CF2 CHBrF 或 CC1FCHC1F ; 三氟甲基為待佳者。 直鍵(Ci - C4 )次烷基二氧基為KHz -O-CH2 CH2 -O-CH2 CHZ CHZ -0-或-O-CH2 CH2 CH2 ch2 -〇〇 芳基為,例如苯基或萘基,特別是苯#。 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再填寫本頁) 雜琛基為5到7員之含1到3值選自包括氮,氣和硫 組群之雜原子之芳香糸或非芳番条琛。較佳為含餌原子為 雜原子之芳番条5和6員琛,合適者含其它雜原子,較佳 為氮或硫,特別是氮。 由R3和—起輿其所鍵結的氡原子形成的5到7 員琛一詞特別是包括吡咯烷•哌啶,嗎啉,硫《啉,六次 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央標隼局員工消費合作社印製 A7 B7 五、發明説明(έ ) 甲基胺,眯唑,吡唑,吡咯,1, 2, 4 —三唑,1, 2 ,3 —三唑,四畦•異噁唑,噁唑,異噁唑啉,嗯唑烷, 睡唑,異睡唑和異嗡唑烷。 本發明範園中較佳者為 (1 )式I化合物,其中 a ) X為氮原子和 Y 為 0CH3 或 NHCH3 或 b ) X為C Η和 Υ 為 0 C Η 3 , 其中: Α為氣原子或NR4基;Alkane 4 CI 1 C This paper scale is applicable to the Chinese National Standard (CNS) M specifications (210X297 mm) 5. Description of the invention (work) A7 B7 Printed base 9 (C 1 1 C 4) for the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Hospital gas group 9 (C 1 — CZ) Binyl group 9 (C 1 — CZ) Halo group gas group »(C 3 — C 6) Alkenyl group (C 3 — C 6) Alkynyl group • (C 1 — C 4) secondary house base two gas base »Radon or nitro 1 η is 0 * 1 2 $ 3 or 4 * ZO is — 0 — • — 0 one (C 1 — C 4) hospital base —» — ( C 1 — C 4) Alkyl 0-0 9 — S (0)-(C! -C 4) Alkyl — S (〇)-~ 9 -S (Ο) S — (C 1 — C 4) Alkyl Base — »m is 0 • 1 9 or 2 t B is (C 1 — C 6) hospital base • halogen one (C 1 — C 6) hospital base 9 (C 3 — C 6) Hunyuan base • or is ( CZ — C 6) Alkenyl or (C 2 — C 4) Alkynyl — (C 1 — C 2) Alkyl »Each is unsubstituted or substituted by 1 to 3 halogens Substituted, or aryl or heteroalkenyl, its white is independently unsubstituted or (C 1 — C 6) alkyl »halogen — (C — C 6) alkyl &gt; halogen» (C 1 — C 6 ) Yuan «radical or halogen — (C 1 — C 6) Yuan oxy mono-substituted to penta-substituted • or R5 .r7 — (CH) -A &lt; 1 Λ, r8 or trimethylsilyl» R 5 $ R 6 $ R 7 9 R 8 and R 9 are white and stand for hydrogen $ (c — C 4) Yuan or halogen $ and P are 0 9 1 9 2 or 3 1 -8- — ^ ---- --AI 装 ------ 定 ----- ί line (please read the precautions on the back before filling in this page) This paper scale is applicable to China National Standard (CNS) 84 specifications (210Χ297mm) Economy A7 ______B7_ printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Education. 5. Description of invention (j) R3 is hydrogen, (Ci _C6) alkyl, (C, -ce) haloalkyl containing 1 to 5 halogen atoms, (Ci- C4) Alkane-based (Ci — C2) hospital base, (Cz — C *) suspected-based (Ci — C2) hospital base It is like unsubstituted or substituted by 1 to 3 yttrium atoms, (C2 — C4) alkynyl mono (Ci _C2) alkyl, unsubstituted or substituted by 1 to 4 halo atoms (C3 _Ce) Chen alkyl , Unsubstituted or substituted by 1 to 4 halogen atoms (C3 — C6), alkynyl (Ci -C4), alkynyl (Cl — C4) halide; (Cl — C4) burned gas Carbonyl- (Ci- (: 2) alkyl, (Ci-c4) alkylaminocarbamate-(Cl-C2) yalkenyl "phenyl- (Ci-C3) courtyard group • Its image is unsubstituted or substituted Halogen, (Cl-c3) alkyl, (Ci _C4) alkane, (Ci -c4) haloalkyl, trityl, nitro or (Ci _C4) subalkyl di-air, their phenyl groups are the same Or different substituents are mono-substituted to tri-substituted; unsubstituted phenyl group or by a self-contained (C! -C4) alkyl group, (Ci -C4) alkane group, halogen, containing 1 to 3 halo Atomic (Ci —C2) haloalkyl, nitro or phenyl monosubstituted or disubstituted phenyl, or unsubstituted pyridyl or independently substituted (Ci _C4) alkyl, (Ci _C4) alkyl Oxygen, halogen, (Ci 〇2) containing 1 to 3 decanolin atoms Alkyl, nitro or pyridyl mono- or di-substituted; R4 is (Ci-C4) alkyl, phenyl, or R3 and R4-together with the nitrogen atom to which they are bonded to form a saturated or unsaturated From 5 to 7 members, this paper is not replaced or is (Ci _C4) alkyl. The paper standard is applicable to China National Standard (CNS) Α4 specification (210X297 mm) ------ Μ 1 装 ----- -Subscribe ----- (Line (please read the notes on the back before filling in this page) A7 B7 printed by the Consumer Cooperative of the Central Bureau of Economic Affairs of the Ministry of Economic Affairs V. Invention description (&gt;) Substituent substitution, may contain 1 To 3 hire extra gas, gas and sulfur heteroatoms. The compound of the present invention possesses the characteristics of killing poems, killing niches and killing codlings. It is suitable as an active ingredient in the fields of agriculture, gardening and physiology. The present invention further includes a method for preparing the compound of the present invention, as well as a composition for killing microbes, killing cockroaches and killing Kundian, the composition containing the compound as an active ingredient, and both the compound and the composition In the control of phytopathogenic emblem bacteria, Chi Yan and Kun niches and prevent such attacks. If the compound of formula I contains an asymmetric sulfon atom, the compound exists in an optically active form. In any case, this compound exists in the form of [E] and / or [Z], only because of the presence of fatty bars, glucosamine and hydrazono double bonds. Furthermore, atropisoieris (atropisoieris ·) may also be present. Formula I is intended to include all possible isomeric forms and mixtures thereof, such as racemic mixtures and any [E / Z] mixtures. Unless specifically defined, the definitions of the terms used above and below are as follows: halogen is fluorine, atmosphere, bromine or iodine, and it is fluorine, chlorine or bromine, and more particularly fluorine or gas. Alkyl is straight chain, such as methyl, ethyl, n-propyl, n-butyl, n-hexyl, n-octyl, n-decyl, n-dodecyl, n-hexadecyl or n-octadecyl, or branched , Such as isopropyl, isobutyl, secondary butyl, tertiary butyl, isopentyl, neopentyl or isohexyl. The alkenyl group is a straight chain or branched carp alkenyl group, such as vinyl, 1_methylvinyl-10-This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (2 丨 0X297mm) I: ------ Jkl installation ------ order ----- (line (please read the precautions on the back before filling in this page) 304860 _ ^ ___ 5. Description of the invention (gray) base, allyl, ι_butene Group, isopropenyl, especially propyl. Alkynyl is, for example, ethynyl, 1-propynyl or 1-butynyl • especially propynyl. It should be understood that cycloalkyl is propyl, butyl , Pentyl or quasi-hexyl substituents such as haloalkyl and haloalkyl gas groups may be partially or completely substituted with the same or different chemical radicals. Examples of haloalkyl groups are gas, ammonia and / or o Mono-substituted to tri-methyl group, such as CHF2, CFs or CHCU; mono-substituted with fluorine, ammonia and / or bromine to penta-substituted ethyl • For example, Cli2 CF3 'CF2 CF3. CF2 CCI3, CF2 CHC12, CF2 CCI3, CF2 CHC1 2. CF 2 CHF e, CF z CFClz, CH2 CHz Cl, CFz CHBr2 · CFz CHC1F, CF2 CHBrF or CC1FCHC1F; trifluoromethyl is preferred. Direct bond (Ci-C4) Subalkyldioxy KHz -O- CH2 CH2 -O-CH2 CHZ CHZ -0- or -O-CH2 CH2 CH2 ch2 -〇〇Aryl is, for example, phenyl or naphthyl, especially benzene #. Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please Read the precautions on the back and then fill out this page.) Zachenji is a 5 to 7 member with 1 to 3 values selected from the group consisting of nitrogen, gas and sulfur groups of heteroatoms of aromatic or non-aromatic fan. Preferably It is a 5th and 6th member of Fenbiao containing bait atoms as heteroatoms, suitable ones contain other heteroatoms, preferably nitrogen or sulfur, especially nitrogen. It is formed by R3 and the radon atom bonded to it The term 5 to 7 Yuanchen especially includes pyrrolidine, piperidine, morpholine, sulfur, and oxoline, six times. This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm). Employee consumption of the Central Standard Falcon Bureau of the Ministry of Economic Affairs Printed by the cooperative A7 B7 V. Description of the invention (έ) Methylamine, zirconium, pyrazole, pyrrole, 1, 2, 4-triazole, 1, 2, 3-triazole, tetrazolium • isoxazole, oxazole Azole, isoxazoline, oxazolidine, oxazole, isoxazole and isoxazolidine. Preferred in the scope of the present invention are (1) compounds of formula I, in which a) X is a nitrogen atom and Y Is 0CH3 or NHCH3 or b) X is C Η and Υ is 0 C Η 3, where: Α is a gas atom or NR4 group;

Ri為氫· (Ci—C4)院基,窗素一(Ci— c4)烷基,琛丙基,m基或甲基硫基;Ri is hydrogen · (Ci-C4) courtyard group, window element one (Ci-c4) alkyl group, propyl group, m group or methylthio group;

Rz為氫,(Ci -C6 )烷基(C3 — C6 )琛烷Rz is hydrogen, (Ci -C6) alkyl (C3-C6) Chenane

η 或噻盼基; D為相同或不同者,其為鹵素· (Ci _C4 )烷基 ,(Ci-C4)烷氧基,(Ci-c2)鹵烷基, ((:1一(:2)豳烷氣基,(〇3—(:6)烯氣基,(C3 一C6)炔氣基,(Cl-C4)次烷基二氣基,氰基或 硝基; -12- 本紙張尺度適用中國國家標隼(CNS ) A4規格(210X297公釐) I 1· 〜 丨裝 訂 ( 線 (請先閱讀背面之注意事項再填寫本頁) ^4860 _&quot;l 五、發明説明(Ί ) η 為 〇, 1,2,3 或 4; 冗為_〇一,一 0 — (Ci 一(:4)烷基一,-(c^ —C4 )院基一 〇 — , - S (Ο) B-, - (Cl - C 4 ) 烷基一S (0) - , - S (Ο) B- (Cl - C 4 )烷基 一&quot;· m 為 0,1 » 或 2 , B為(C! _C6 )烷基•豳一 (Ci _C6 )烷基 ,(C3 _C6 )琿烷基,或為(Cz - C6 )烯基或( C2 — C4 )炔基一 (Ci —C2 )烷基,毎鴒未被取代 或被1到3錮鹵原子取代,或為芳基或雜琛基,其艟自 «立地未被取代或被(Ci —Ce )烷基·鹵素一 (Ci -c6 )烷基,鹵素,(Ci 一(:6 )烷氧基或if素一(η or thienyl; D is the same or different, which is halogen · (Ci _C4) alkyl, (Ci-C4) alkoxy, (Ci-c2) haloalkyl, ((: 1 1 (: 2 ) Binane gas group, (〇3-(: 6) alkene gas group, (C3-C6) alkynyl gas group, (Cl-C4) hypoalkylene gas group, cyano or nitro; -12- this paper The standard is applicable to China National Standard Falcon (CNS) A4 specification (210X297 mm) I 1 · ~ 丨 binding (line (please read the precautions on the back before filling in this page) ^ 4860 _ &quot; l V. Description of invention (Ί) η Is 〇, 1, 2, 3 or 4; redundant is _〇 one, a 0 — (Ci one (: 4) alkyl one,-(c ^ — C4) yard group one — — S (Ο) B -,-(Cl-C 4) alkyl mono S (0)-,-S (Ο) B- (Cl-C 4) alkyl mono &quot; · m is 0, 1 »or 2, B is (C ! _C6) alkyl • Ci_C6) alkyl, (C3 _C6) eunyl, or (Cz-C6) alkenyl or (C2 — C4) alkynyl- (Ci —C2) alkyl, each The tungsten is unsubstituted or substituted with a halogen atom of 1 to 3, or is an aryl group or a heteroalkenyl group, and its base is unsubstituted or substituted by (Ci —Ce) alkyl · halogen mono (Ci -c6) alkyl ,halogen , (Ci one (: 6) alkoxy or if element one (

Ci-Cs)烷基單取代到五取代,或為Ci-Cs) alkyl mono to five substitutions, or

(請先聞讀背面之注意事項再填寫本頁) R/ r8 R 5 , R 6 , R 7 , Rs和R9镰自»立為鬣,(Ci(Please read the precautions on the back and then fill out this page) R / r8 R 5, R 6, R 7, Rs and R9 Sisi stand up as Hyena, (Ci

經濟部中央揉準局員工消費合作社印IPrinted by the Immigration and Consumer Cooperative of the Central Ministry of Economic Affairs

子 C 烷 4 原 ί &gt; I 到 歯 I Ζ 2 1 偏基 c C 被 5 氣 I ί 或 到烷 1 , 代 1 } C 代取 含 4 ί 取被 ,C I 子未 基 I 基原. 烷-烯由基 } C _ «烷 6 (43) ;c , C 到 2 和 3 I 基 I 1 C , 或-烷 2 被 I 素 2 C 鹵 C 或 -a , ί &gt; &lt; 代 C 或 1 * 6 .取 { 基 ,氫 C 基被 I 燒 ο 為 1 烷未基 &gt; 為 3 1 } 你快 4 p R C 2 其} c ( C · 4 1 的一基 C 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(方) 鹤鹵原子取代的(C3 —(:6 )琛烷基•未被取代或被1 到4偁鹵原子取代的(C3 — C6 )琛烷基一(Ci 一0:4 ) 烷基,«基一 (Ci—C*)烷基;(Ci—Ci)烷 氣基羰基一 (Ci-Cz)烷基.苯基一 (Cl_C3) 烷基,其你未被取代或被由素,(Ci — C3 )烷基, (Ci— C4)烷氣基,(Ci— c4)鹵烷基,氣基, 硝基或(Ci —c4 )次烷基二氣基取代,其苯基被相同 或不同取代基單取代到三取代;未被取代的苯基或被《自 «立被(Ci-C*)烷基,(Ci_C4)烷氣基•鹵 素,含1到3镳鹵索原子的(Ci _C2 )崮烷基,硝基 或氱基單取代或二取代的苯基,或未被取代的吡啶基或被 镳自獮立被(Ci— C4)烷基,(Ci—C*)烷氣基 ,豳素,含1到3镅鹵素原子的(Ci _C2 )鹵烷基, 硝基或氣基單取代或二取代的吡啶基; R4為(C! 一04 )烷基,苯基,或 R3和R4 —起與其所鍵結的氮原子形成飽和或不飽 和之5到7員環,該琛未被取代或被(Ci -C4 )烷基 取代基取代,可含1到3健額外的遘自氮,氣和硫之雜原 子。 (2) 式I化合物,其中X為氮· Y為〇CH3 ; (3) 式I化合物,其中X為CH ; (4) 式I化合物,其中X為N, Y為NHCH3 , 為H, CH3 ,環丙基或CN; -14- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I,------Jk—裝------訂-----&lt; 線 (請先閲讀背面之注意事項再填寫本頁) 304860 A7 B7 五、發明説明(?) (5) 式I化合物,其中A為氣,NCH3或n-C6 Hs •特別是氣或NCHs ,更待別是氣; (6) 式I化合物,其中Ri為氫,甲基•環丙基或気基 ,持別是甲基; (7) 式I化合物,其中R2為(Ci 一 C4 )烷基或琛 丙基,特別是甲基或琛丙基; 2 為 8)式I化合物,其中R2為 一/~^&gt; 和 D基為曲素,(Ci—CU)烷基,(Ci_C4) 烷氣基,被1到5悃鹵原子取代的(Ci 一02 )烷基, C2)豳烷氧基,(C3 —Ce)烯氣基,(C3Subalkane 4 original ί &gt; I to 歯 I Z 2 1 partial group c C is 5 gas I ί or to alkane 1, generation 1} C is substituted with 4 ί taken, CI is not based on I base. Alkyl -Alkenyl group} C _ «alkane 6 (43); c, C to 2 and 3 I group I 1 C, or-alkane 2 is halogenated by I element 2 C or -a, ί &gt; &lt; instead of C or 1 * 6. Take {group, hydrogen C group is burnt by I ο 1 alkyl group> 3 1} You are fast 4 p RC 2 its} c (C · 4 1 of a base C This paper size is suitable for China Standard (CNS) Α4 specification (210 × 297 mm) A7 B7 printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of the Invention (Party) (C3 — (: 6)) alkyl substituted by a halogen atom • Not substituted or (C3-C6) alkyl (Ci-C 0: 4) alkyl substituted with 1 to 4 halogen atoms, «Ci- (Ci-C *) alkyl; (Ci-Ci) alkanoylcarbonyl- (Ci-Cz) alkyl. Phenyl- (Cl_C3) alkyl, which is unsubstituted or substituted by element, (Ci—C3) alkyl, (Ci—C4) alkyl, (Ci—c4) halogen Alkyl, gas, nitro or (Ci —c4) hypoalkyl digas, the phenyl group is the same or different Substituted groups are mono- to tri-substituted; unsubstituted phenyl groups or "self-supported (Ci-C *) alkyl groups, (Ci_C4) alkanoyl groups • halogens, containing 1 to 3 ammonium halide atoms (Ci _C2) Phenyl, nitro or phenyl mono- or di-substituted phenyl, or unsubstituted pyridyl or (Ci-C4) alkyl, (Ci-C *) alkane Group, bismuth, (Ci _C2) haloalkyl containing 1 to 3 americium halogen atoms, nitro or gas-based mono- or di-substituted pyridyl; R4 is (C!-04) alkyl, phenyl, or R3 and R4 together form a saturated or unsaturated 5- to 7-membered ring with the nitrogen atom to which they are bonded. This is unsubstituted or substituted with a (Ci -C4) alkyl substituent, which may contain 1 to 3 additional It is a heteroatom of nitrogen, gas and sulfur. (2) Compound of formula I, where X is nitrogen · Y is 〇CH3; (3) Compound of formula I, where X is CH; (4) Compound of formula I, where X is N, Y is NHCH3, H, CH3, cyclopropyl or CN; -14- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) I, ------ Jk-installed- ---- order ----- &lt; line (please read the notes on the back before filling this page) 30 4860 A7 B7 5. Description of the invention (? ) (5) Compound of formula I, where A is gas, NCH3 or n-C6 Hs • Especially gas or NCHs, not to mention gas; (6) Compound of formula I, where Ri is hydrogen, methyl • cyclopropyl Or protyl, which is otherwise methyl; (7) The compound of formula I, wherein R2 is (Ci-C4) alkyl or propyl, especially methyl or propyl; 2 is 8) The compound of formula I, wherein R2 is mono / ~ ^> and the D group is kojirin, (Ci_CU) alkyl, (Ci_C4) alkanoyl, (Ci-02) alkyl substituted with 1 to 5 halogen atoms, C2) 豳Alkoxy, (C3-Ce) alkenyl, (C3

(C —Ce )炔氧基· (Ci -C4 )次烷基二氧基,镢基或 硝基,或嚐盼基; D特別是氟,氯,溴(C -Ce) alkynyloxy · (Ci -C4) alkylidene dioxy, phenyl or nitro, or trypanyl; D is especially fluorine, chlorine, bromine

Ci _C4 )烷基或一 CF3Ci_C4) alkyl or one CF3

Z-B (9)式I化合物,其中R2為 IJ------{ , I裝------訂-----f 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局貝工消費合作社印製 (D) Ζ 為 — 0 — f — 0 -( C 1 一 C 4 )院基— 9 一 (C — C 4 ) 院 基 — 0 一 ,-S ( 0 ) Ζ — ,-(C 1 — C 4 烷 基 — S ( 〇 ) 2 一 .—S ( 〇 ) Ζ 一 (C !- C 4 )烷 基 — 9 待 別 是 — 0 — • — C Η 2 — 0 — 或_ 0 - C Η 2 — • 更 特 別 是 — 0 — C Η ζ ; ( 1 0 ) 式 I 化 合 物 ,其中 R 2 為 &lt;5 Ζ- Β 15- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7ZB (9) Compound of formula I, where R2 is IJ ------ {, I loaded ------ ordered ----- f line (please read the notes on the back before filling this page) Economy Printed by the Beigong Consumer Cooperative of the Ministry of Central Standards (D) ZO is — 0 — f — 0 — (C 1 — C 4) courtyard — 9 — (C — C 4) courtyard — 0 one, -S (0 ) AZ —,-(C 1 — C 4 alkyl—S (〇) 2 one.—S (〇) ZO— (C!-C 4) alkyl— 9 Wait until it is — 0 — • — C Η 2 — 0 — or _ 0-C Η 2 — • More specifically — 0 — C Η ζ; (1 0) Compounds of formula I, where R 2 is &lt; 5 ZO- Β 15- This paper scale is applicable to Chinese national standards ( CNS) A4 specification (210X297mm) A7

經濟部中央標準局員工消費合作杜印裝Du Printing Co., Ltd. Employee Consumption Cooperation of Central Bureau of Standards of the Ministry of Economic Affairs

五、發明説明(/。) B為(Ci 一 C4 )院基,由—(Ci —C4 )院基 •或為(C2 — C4 )烯基或(C2 _C4 )炔基_ (Ci -C2)烷基,毎β未被取代或被1到3儀由原子取代, 或為芳基或籲自》立地未被取代或被(Ci _c2 )烷基 .鹵素一 (Ci -Cz )烷基·豳索,(Ci — C2 )烷 氧基或鹵素一 (c1—Cz)烷基單取代到二取代,或為Fifth, the description of the invention (/.) B is the (Ci-C4) hospital base, consisting of (Ci-C4) hospital base or (C2-C4) alkenyl or (C2_C4) alkynyl_ (Ci-C2) Alkyl, β is unsubstituted or substituted by 1 to 3 atoms by atoms, or is aryl or voluntarily, unsubstituted or substituted by (Ci _c2) alkyl. Halogen one (Ci -Cz) alkyl · bin Cable, (Ci-C2) alkoxy or halogen mono- (c1-Cz) alkyl mono- to di-substituted, or

R 5 , R 6 , R 7 , Re和R9®自獼立為氫,(Ci 一C2)烷基或鹵素,和 P 為 0 , 1 , 2 或 3 ; B待別是(Ci 一〇2)烷基•鹵一 (Ci _C3 ) 烷基,或為烯丙基或炔丙基,毎《未被取代.或在所有情 況下被1或2雇鹵原子或1或2楢甲基取代,或苯基,被 —傾選自氟,氰,溴和CF3之取代基取代,或為 —(CH)2 (1 1)式I化合物,其中Rz為4 —位置被一 Z — B取 代的苯基; (12)式I化合物,其中 R3為氫,(Ci -C6 )烷基,含1到3偏鹵原子 的(Ci -C4)窗烷基,(Ci _C2)烷氣基一( _ 1 6 _ 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I; { I裝 訂 f 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(M )R 5, R 6, R 7, Re and R9® are selected from hydrogen to hydrogen, (Ci-C2) alkyl or halogen, and P is 0, 1, 2 or 3; B to be (Ci-〇2) Alkyl • Halogen (Ci _C3) alkyl, or allyl or propargyl, which is unsubstituted. Or in all cases substituted by 1 or 2 halogen atoms or 1 or 2 methyl groups, or Phenyl, substituted by a substituent selected from fluorine, cyanide, bromine and CF3, or — (CH) 2 (11) compound of formula I, where Rz is a phenyl substituted at the 4-position by a Z—B (12) The compound of formula I, wherein R3 is hydrogen, (Ci-C6) alkyl, (Ci-C4) window alkyl containing 1 to 3 partial halogen atoms, (Ci _C2) alkane group (_ 1 6 _ This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) I; {I binding f line (please read the precautions on the back before filling this page) A7 B7 printed by the Employee Consumer Cooperative of the Central Bureau of Standards V. Description of Invention (M)

Ci— C2)烷基,(C^-CU)烷氣基羰基一 (C, —CZ)烷基,未被取代或被1到3镳曲原子取代的丙烯 基,烯丙基,(C3-Ce)琛烷基,未被取代或被1到 2掴鹵原子取代的璨丙基甲基,氟基一 _CZ )烷 基,未被取代或被鹵素,甲基,甲氣基或含1到3籲鹵原 子取代的苯基一 (Ci — C2 )烷基,苯基可能未被取代 或被相同或不同取代基取代;未被取代的苯基或被鵪自》 立被(C! — C4 )烷基· (Ci 一匚4 )烷氣基,鹵素 ,含1到3梅齒素原子的(Ci — C2 )鹵烷基,硝基或 «基單取代或二取代的苯基,或未被取代的毗啶基或被艟 自獼立被(C! — C4 )烷基,(C! _C4 )烷氣基, 鹵素,含1到3傾鹵素原子的(C1 -C2 )鹵烷基,硝 基或氰基單取代或二取代的吡啶基;或R3和R4 —起與 其所鍵結的氮原子形成飽和或不飽和之5到7員琢,該琛 未被取代或被(Ci _C4 )烷基取代,可含1到3催額 外的遘自氮,氧和硫之雜原子; R3較佳為氳,(〇1—06)烷基,含1到3值鹵 原子的(Ci —C4 )成院基,(Ci —Cz )焼氣基甲 基,未被取代或被1到3®鹵原子取代的丙一 2_烯一 1 一基,烯丙基,(C3 — C6&gt;琛烷基,未被取代或被1 到2個氟或氯原子取代的環丙基甲基,氱基—(Ci _CZ ) 烷基,未被取代或被鹵素,甲基,甲氣基或含i到3雇鹵 原子取代的鹵甲基取代的苯基一 _C2 )烷基,苯 -17- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 丨:------&lt; I裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 ____B7_ 五、發明説明(/工) 基可能未被取代或被相同或不同取代基單取代到二取代; 未被取代的苯基或被籲自猻立被鹵素,甲基,甲氣基,含 1到3鏑豳原子的鹵甲基,氣基或硝基取代苯基;未被取 代的tt啶基或被籲自獨立被鹵素,甲基,甲氣基,含1到 3艏齒原子的鹵甲基,氡基或硝基取代吡啶;或r3和 R4 —起與其所鍵結者為1, 2, 4 —三唑基,4— «I淋 基·1一氮雜草基,1一哌啶基或1一吡咯烷基, R 3特佳為甲基; (13) 式I化合物,其中R4為甲基或苯基,特別是甲 基; (14) 式I化合物,其中 X為CH;Y為OCH3 ;Ri為CH3 ;A為氣; R2為4 一甲基苯基或4 一烯丙氣基苯基或4_ (3 一三氟甲基一苄氣基)苯基或4一 (2, 2—二氣琛丙基 甲氣基 &gt; 苯基和 R 3 為 C Η 3 ; (15) 式I化合物,其中 a ) X為氮原子和 Y 為 0CH3 或 NHCH3 或 b ) X為C Η和 Υ 為 0 C Η 3 . 其中: Α為氣原子或NR4基; -18- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 17 n 人 &quot;&quot;裝 訂 ( 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(丨3 )Ci— C2) alkyl, (C ^ -CU) alkylcarbonylcarbonyl mono (C, —CZ) alkyl, propenyl, allyl, unsubstituted or substituted by 1 to 3 amino atoms, (C3- Ce) Chen alkyl, unsubstituted or substituted with 1 to 2 slap halogen atom, propylmethyl, fluoro-CZ) alkyl, unsubstituted or halogen, methyl, methyl group or containing 1 To the phenyl mono (Ci — C2) alkyl substituted by 3 halogen atoms, the phenyl group may be unsubstituted or substituted by the same or different substituents; the unsubstituted phenyl group may be substituted by quaternity (C! — C4) Alkyl (Ci- 匚 4) alkane, halogen, (Ci — C2) haloalkyl containing 1 to 3 mesitine atoms, nitro or phenyl mono- or di-substituted phenyl, or Unsubstituted pyridinyl or sulfonated (C! — C4) alkyl, (C! _C4) alkane, halogen, (C1 -C2) haloalkyl containing 1 to 3 tilt halogen atoms , Nitro or cyano mono- or di-substituted pyridyl; or R3 and R4 together with the nitrogen atom to which they are bound to form a saturated or unsaturated 5 to 7 member, the Chen is not substituted or (Ci _C4 ) Alkyl substitution, may contain 1 to 3 additional nitrogen Heteroatoms of oxygen and sulfur; R3 is preferably radium, (〇1-06) alkyl, (Ci-C4) containing 1 to 3 halogen atoms to form a hospital group, (Ci-Cz) halomethyl, Unsubstituted or substituted with 1 to 3® halogen atoms propa-2-en-1-yl, allyl, (C3-C6) alkyl, unsubstituted or substituted with 1 to 2 fluorine or chlorine atoms Cyclopropylmethyl, propyl- (Ci _CZ) alkyl, unsubstituted or substituted by halogen, methyl, methyl, or halogenated methyl substituted with halogen atoms containing 1 to 3 halogen atoms —C2 ) Alkyl, Benzene-17- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X 297mm) 丨: ------ &lt; I installed ------ ordered ----- f line (please read the precautions on the back before filling in this page) A7 ____B7_ printed by the employee consumer cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Invention description (/ work) The group may not be substituted or be replaced by the same or different substituents. Disubstituted; unsubstituted phenyl or thiophene is substituted by halogen, methyl, mesyl, halomethyl containing 1 to 3 dysprosium atoms, phenyl or nitro; unsubstituted ttPyridyl or be called alone Substituted pyridine by halogen, methyl, methyl group, halomethyl containing 1 to 3 bow tooth atoms, radon or nitro; or r3 and R4 together with it is 1, 2, 4-triazole Group, 4— «Ilinyl · 1 azepine, 1 piperidinyl or 1 pyrrolidinyl, R 3 is particularly preferably methyl; (13) The compound of formula I, wherein R 4 is methyl or benzene Group, especially methyl; (14) Compound of formula I, wherein X is CH; Y is OCH3; Ri is CH3; A is gas; R2 is 4-methylphenyl or 4-allylaminophenyl or 4- (3 monotrifluoromethyl monobenzyl) phenyl or 4- (2, 2-difluoromethylpropyl) phenyl and R 3 is C Η 3; (15) The compound of formula I, wherein a) X is a nitrogen atom and Y is 0CH3 or NHCH3 or b) X is C Η and Υ is 0 C Η 3. Among them: Α is a gas atom or NR4 group; -18- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 17 n people &quot; &quot; binding (line (please read the precautions on the back before filling out this page) A7 B7 printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economy V. Invention description (丨 3)

Ri為氫,(Ci 一〇4 )烷基·琛丙基,氱基或甲 基硫基;Ri is hydrogen, (Ci 104) alkyl · propyl, propyl or methylthio;

Rz 為氫;(Cj—Ce)烷基;(C3-C6)琛 烷基;未被取代的苯基或被籲自獨立被曲索,(C I -C4)烷基,(Ci—C*)烷氣基,(Ci-Cz)曲 烷基,(Ct—Cz)鹵烷氱基· (C3— C6)烯基氧 基,(C3— Ce)烯基氣基,(Ci_C4)次氣基二 氣基,硝基或氣基單取代或二取代的苯基;或β吩基; R3為氫,((:1一0:6)烷基,含1到5籲曲原子 的(Ci — Ce )齒院基· (Ci —C4 )院氣基一(Ci 一 C2 )烷基,(C2 _C4 )烯基一(Ci _c2)烷 基,其你未被取代或被1到3«鹵原子取代,(C2— C4 )炔基一 (Ci -C2 )烷基,未被取代或被1到4 镳鹵原子取代的(Cs _C6 )環烷基,未被取代或被1 到4鴒鹵原子取代的(C3 — Ce )琛烷基一 (Ci — C4 ) 烷基,氣基一 (Ci-C^)烷基;(Ci 一 C4)烷氣 基羰基—(Ci —C2 )烧基,苯基一(Cl _C3 )院 基,其你未被取代或被鹵素,(Ci_C3)烷基,(Ci _C4)烷氣基,(Ci— C4)鹵烷基,氛基,硝基或 (Ci _C4 )次烷基二氣基取代,其苯基被相同或不同 取代基單取代到三取代;未被取代的苯基或被縝自》立被 (Ci— C4)烷基,(Ci-C*)烷氧基.曲素,含 1到3値鹵素原子的(Ci -C2 )曲烷基.硝基或氮基 -19- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ------{、I裝------訂-----^線 (請先閱讀背面之注意事項再填寫本頁) A7 B7 3〇486〇 ^------- 五、發明説明(w) 單取代或二取代的苯基,或未被取代的吡啶基或被籲自獨 立被(Ci —C4 )烷基,(C! — C4 )烷氣基,鹵素 ,含1到3鍺鹵素原子的(Ci -CZ )鹵烷基,硝基或 氱基單取代或二取代的吡啶基; R4為(Ci 一 C4 )烷基,苯基,或 R3和R4 —起與其所鐽結的氮原子形成飽和或不餡 和之5到7員琛,該琛未被取代或被(C^ _C4 )烷基 取代基1,可含1到3傾額外的灌自氮,氣和硫之雜原子 〇 (16)式I化合物,其中 X為C Η或N Υ 為 0 C Η 3 Α為0或N-R4 Ri為甲基,環丙基或甲基硫基;Rz is hydrogen; (Cj—Ce) alkyl; (C3-C6) alkyl; unsubstituted phenyl or benzoxine, (CI -C4) alkyl, (Ci—C *) Alkyl group, (Ci-Cz) trekyl group, (Ct-Cz) haloalkane group · (C3-C6) alkenyloxy group, (C3-Ce) alkenyl group, (Ci_C4) sub-gas group Gas group, nitro group or gas group mono- or di-substituted phenyl group; or β phenyl group; R 3 is hydrogen, ((: 1 a 0: 6) alkyl group, containing 1 to 5 Yuqu atoms (Ci — Ce ) Dental hospital group · (Ci — C4) hospital gas group one (Ci — C2) alkyl, (C2 _C4) alkenyl one (Ci _c2) alkyl, which you are not substituted or substituted by 1 to 3 «halogen atoms , (C2-C4) alkynyl mono (Ci-C2) alkyl, (Cs _C6) cycloalkyl unsubstituted or substituted by 1 to 4 hydrogen atoms, unsubstituted or substituted by 1 to 4 halide halogen atoms (C3-Ce) Chen-alkyl (Ci-C4) alkyl, gas-Ci-C ^ alkyl; (Ci-C4) alkanecarbonyl-(Ci-C2) alkyl, phenyl A (Cl _C3) group, which is unsubstituted or halogenated, (Ci_C3) alkyl, (Ci _C4) alkane, (Ci-C4) haloalkyl, atmosphere, nitro (Ci _C4) Subalkyl diamino group, the phenyl group of which is mono- to tri-substituted by the same or different substituents; the unsubstituted phenyl group is or is substituted by (Ci-C4) alkyl, (Ci -C *) alkoxy. Kojirin, (Ci -C2) kojitan.nitro or nitrogen group containing 1 to 3 halogen atoms -19- This paper scale is applicable to China National Standard (CNS) A4 specification (210X297 Mm) ------ {, I installed ------ ordered ----- ^ line (please read the notes on the back before filling this page) A7 B7 3〇486〇 ^ --- ---- V. Description of the invention (w) Mono-substituted or di-substituted phenyl, or unsubstituted pyridyl or independently (Ci — C4) alkyl, (C! — C4) alkane , Halogen, (Ci-CZ) haloalkyl containing 1 to 3 germanium halogen atoms, nitro or phenyl mono- or di-substituted pyridyl; R4 is (Ci-C4) alkyl, phenyl, or R3 and R4-form a saturated or unfilled nitrogen atom with the nitrogen atom to which it forms 5 to 7 members, which is unsubstituted or substituted with (C ^ _C4) alkyl substituent 1, which may contain 1 to 3 additional A heteroatom from nitrogen, gas and sulfur 〇 (16) Compound of formula I, where X is C Η or N Υ is 0 C 3 Α is 0 or N-R4 Ri is methyl, cyclopropyl or methylthio;

Rz為甲基;琢丙基;未被取代的苯基或玀立被鹵素 .(Ci 一 C4)院基,(Ci 一 C4)院氣基,1 到 5 籲鹵原子取代的(Ci _c2 )烷基,(Ci 一c2 &gt; ϋ 烷氣基· (〇3-(:6)烯氧基,(c3-c6)炔氣基 ,(Ci-Ci)次烷基二氧基,氡基或硝基單取代到二 取代的苯基,或鼴吩基;其中 R 3定義同式I和 R4為甲基或苯基,或 R3和R4 —起與其所鍵結的氮原子為吡咯烷,哌淀 -20- 本紙張尺度適用中國國家標準(CNS )八4規格(210X297公釐) —.I------人一裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 經濟部中央標準局貝工消費合作社印製 A7 B7 五、發明説明(ο ,嗶啉,硫梅啉,六次甲基亞胺,味唑,毗唑,吡咯,1 • 2, 4-三唑或1, 2, 3-三睡。 (17) 式I化合物,其中 X為Ν , Υ 為 N H C Η 3 · Α 為 0 或 N—R4 ,Rz is a methyl group; a propyl group; an unsubstituted phenyl group or a halogen group. (Ci-C4) group, (Ci-C4) group gas group, 1 to 5 halogen atoms substituted (Ci _c2) Alkyl, (Ci-c2 &gt; ϋ alkynyl · (〇3- (: 6) alkenyloxy, (c3-c6) alkynyl, (Ci-Ci) hypoalkylene dioxy, radon or Nitro mono-substituted to di-substituted phenyl, or molenyl; wherein R 3 is defined as formula I and R 4 is methyl or phenyl, or the nitrogen atom bonded to R 3 and R 4 is pyrrolidine, piper Dian-20- This paper scale is applicable to the Chinese National Standard (CNS) 84 specifications (210X297mm) —.I ------ People Packing ------ Order ----- f line (please Read the precautions on the back first and then fill out this page) Printed by the Ministry of Economy Central Standards Bureau Employee Consumer Cooperatives Printed by the Ministry of Economic Affairs Central Standards Bureau Beigong Consumer Cooperatives A7 B7 Fifth, the invention description (ο, Pyroline, Thiomeline, six Methylimine, azole, pyrazole, pyrrole, 1, 2, 4-triazole or 1, 2, 3-triazole. (17) Compounds of formula I, where X is Ν, Υ is NHC Η 3 · Α Is 0 or N—R4,

Ri為甲基,琛丙基或甲基硫基; R2為甲基;琿丙基;未被取代的苯基或獼立被鹵素 ,(Ci—C*)烷基,(Ci 一 C4)烷氣基,1 到 5 鹤鹵原子取代的(Ci — C2 )烷基,(Ci -CZ )鹵 烷氣基,(C3 —Ce)烯氣基,(C3 -Ce)炔氣基 .(Ci—C*)次烷基二氣基,氱基或硝基單取代到二 取代的苯基,或噻盼基;其中 R 3定義同式I和 R4為甲基或笨基,或 R3和R4 —起輿其所鍵结的《原子為吡咯烷,哌啶 ,瞟啉,硫瞟啉,六次甲基胺,咪唑•吡唑.毗咯,1, 2, 4 —三唑或1, 2, 3 -三唑。 (18) 式I化合物,其中 A為氣, R i為甲基, 為甲基;未被取代的苯基或獼立被鹵素,(Ci -C4 )烷基,(Ct —C4 )烷氣基· 1到5值歯原子 -2 1- 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) ------f I裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央揉準局貝工消費合作社印製 A7 B7 五、發明説明(丨 取代的(Cl -C2 )院基· (Cl — C2 ) 院氣基· (C3—ce)烯氣基,(C3—ce&gt;炔氣基,(Ci -c4)次烷基二氣基,《基或硝基單取代到二取代的苯 基,或嚐盼基;其和 R3 為(Ci — Ce )院基; X和Y定義同式I 〇 (19) 式I化合物,其中 R i為甲基, R 2為甲基,和 R 3如所述, R4為甲基或苯基,或 R3和R4 —起舆其所鍵结的氮原子形成銪和或不飽 和之5到7員環,該琛未被取代或被(Ci _C4 )烷基 取代,可含1到3餹額外的S自氮,氣和硫之雜原子;而 A, X和Y如式I所定義。 (20) 式I化合物,其中 R3為氫;(Ci —C4 )烷基;含1到3镧齒原子 的(Cl —C4 )處焼基;(Cl — C2 )院氣基一( _C2 )烷基;未被取代或被1到3值鹵原子取代的 丙烯基;烯丙基;(C3 _C6 )環烷基;未被取代或被 1到2®鹵原子取代的環丙基甲基;氰基一 (Ci _C2 )院基;(Ci —C2 )焼氣基嫌基一 (Cl —C2 )院 基;未被取代或被鹵素,甲基,甲氣基或含1到3镳鹵原 -22- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ΙΛ------f I裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) ^04860 g ^04860 g 經濟部中央標準局員工消費合作社印製 五、發明説明(Π ) 子,«基,硝基或(Ci 一〇2 )次烷基二氣基取代的苯 基一 (Ci 一 Cz )烷基,苯基可能未被取代或被相同或 不同取代基單取代到二取代;未被取代的苯基或被《自獼 立被鹵素,甲基,甲氣基,含1到3籲鹵原子的崮甲基· 氱基或硝基單取代或二取代的苯基;或未被取代的毗啶基 或被偏自》立被鹵素,甲基,甲氣基,含1到3籲鹵原子 的鹵甲基,氣基或硝基單取代或二取代的毗啶基; R4為甲基或苯基;或 R3和R4 —起輿其所鍵結的氮原子形成鮑和或不飽 和之5到7貝琛,該琛未被取代或被(Ci _C4 )烷基 取代,可含1到3鶴額外的選自氮,氣和硫之雜原子;而 A, X, Y, 如式I所定義。 (21) (20)所提到的式I化合物中,其中Rs和 R4 —起與其所鍵結的氮原子為三唑基,暍啉基,2, 6 -二甲基暍啉基,氮雜革基,衹啶基或吡咯烷基。 (22) 式I化合物,其中 A為氣, R ^為甲基. R 2為甲基;未被取代的苯基或玀立被®素,(C , 一C4)烷基,(C!-C4)烷氣基,1到5錮豳原子 取代的(Ci -C2 )烷基,(C: -C2 )鹵烷氣基, (C3 —Ce)烯氣基,(C3 —C6)炔氣基,(Ci -C4 )次烷基二氣基,氯基或硝基單取代到二取代的苯 -23- 本紙張A度適用中國國家標準(CNS ) A4^格(210X297公釐) I:------' —裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(α) 基,或噻盼基;和 R3為氫;(Ci _C4 )烷基;含1到3籲鹵原子 的(Ci _C4)鹵烷基;(Ci —C2)烷氣基一( C:-Cz)烷基;未被取代或被1到3俪鹵原子取代的 丙烯基;烯丙基;(C3 -C6 &gt;琛烷基;未被取代或被 1到2鏟鹵原子取代的瑷丙基甲基;氯基一 (C i -C2 )烷基;(Ci 一〇2 )烷氣基羰基一 (Ci _C2 )烷 基;未被取代或被鹵素,甲基,甲氣基或含1到3個齒原 子,《基,硝基或(Ct _C2 )次院基二氣基取代的苯 基一 (Ci _C2 )烷基,苯基可能未被取代或被相同或 不同取代基單取代到二取代;未被取代的苯基或被艟自猜 立被鹵素,甲基,甲氣基,含1到3值鹵原子的鹵甲基, 氱基或硝基軍取代或二取代的苯基;或未被取代的吡啶基 或被值自獮立被鹵素,甲基,甲氧基,含1到3健曲原子 的鹵甲基,氰基或硝基單取代或二取代的吡啶基;而X和 Y如式I所定義。 (2 3) (22)所提到的式I化合物,其中: A為氣, R i為甲基,Ri is methyl, propyl or methylthio; R2 is methyl; propyl; unsubstituted phenyl or halide is halogen, (Ci-C *) alkyl, (Ci-C4) alkyl Gas group, (Ci — C2) alkyl substituted with 1 to 5 tungsten halogen atoms, (Ci -CZ) haloalkane group, (C3-Ce) alkenyl group, (C3-Ce) alkynyl group. (Ci— C *) Dialkyl diamino, mono- or nitro mono-substituted to di-substituted phenyl, or thienyl; wherein R 3 is defined as formula I and R 4 is methyl or stupyl, or R 3 and R 4 — "The atom is pyrrolidine, piperidine, oxoline, thioxoline, hexamethyleneamine, imidazole • pyrazole. Pyrrole, 1, 2, 4-triazole or 1, 2, 3-Triazole. (18) The compound of formula I, wherein A is gas, R i is methyl, is methyl; unsubstituted phenyl or halide is halogen, (Ci -C4) alkyl, (Ct -C4) alkyl gas · 1 to 5 values for Atomic-2 1- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ------ f I installed ------ ordered ---- -f line (please read the precautions on the back before filling in this page) A7 B7 printed by the Beigong Consumer Cooperative of the Central Bureau of Economic Development of the Ministry of Economy V. Description of the invention (丨 Replaced (Cl -C2) Hospital Base · (Cl — C2 ) Hospital gas group (C3-ce) alkenyl gas group, (C3-ce> alkynyl gas group, (Ci-c4) hypoalkylene gas group, mono- to di-substituted phenyl group or nitro group, or Tsaipan group; R3 and R3 are (Ci — Ce) group; X and Y are defined as formula I 〇 (19) Formula I compound, wherein R i is methyl, R 2 is methyl, and R 3 is as described , R4 is methyl or phenyl, or R3 and R4-together with the nitrogen atom to which they are bound to form europium and or an unsaturated 5- to 7-membered ring, which is not substituted or substituted by (Ci _C4) alkyl , May contain 1 to 3 extra S heteroatoms from nitrogen, gas and sulfur; and A, X and Y are as shown in formula I (20) The compound of formula I, wherein R3 is hydrogen; (Ci —C4) alkyl; (Cl —C4) alkyl group containing 1 to 3 lanthanide atoms; (Cl — C2) hospital gas group one (_C2 ) Alkyl; unsubstituted or substituted with 1 to 3 halogen atoms; allyl; (C3_C6) cycloalkyl; unsubstituted or substituted with 1 to 2® halogen atoms ; Cyano one (Ci _C2) courtyard group; (Ci — C2) yin gas base group (Cl — C2) courtyard group; unsubstituted or halogenated, methyl, methyl group or containing 1 to 3 ammonium halide Original-22- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) ΙΛ ------ f I installed ------ order ----- f line (please read the back first (Notes to fill out this page again) ^ 04860 g ^ 04860 g Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Invention Instructions (Π), «Base, Nitro or (Ci 〇2) Subalkyl Digas Phenyl- (Ci-Cz) alkyl substituted by phenyl, phenyl may be unsubstituted or mono- to di-substituted by the same or different substituents; unsubstituted phenyl or by "halogenated by halogen, methyl , A gas group, containing 1 to 3 halogen Phenylmethyl, propyl or nitro mono- or di-substituted phenyl; or unsubstituted pyridinyl or partially substituted by halogen, methyl, methyl group, containing 1 to 3 halogen Atom's halomethyl, gas or nitro mono- or di-substituted pyridinyl; R4 is methyl or phenyl; or R3 and R4 together with the nitrogen atom to which they are bound form abalone or unsaturated 5 to 7 Beichen, which is unsubstituted or substituted with (Ci _C4) alkyl, may contain 1 to 3 additional heteroatoms selected from nitrogen, gas and sulfur; and A, X, Y, as in formula I As defined. (21) In the compound of formula I mentioned in (20), the nitrogen atom to which Rs and R4 are bonded together is triazolyl, thoracolinyl, 2,6-dimethyl thoracolinyl, aza Leather base, only pyridyl or pyrrolidinyl. (22) The compound of formula I, wherein A is gas, R ^ is methyl. R 2 is methyl; unsubstituted phenyl or oligotropin, (C, a C4) alkyl, (C!- C4) Alkyl, (Ci -C2) alkyl substituted with 1 to 5 atoms, (C: -C2) haloalkane, (C3-Ce) alkenyl, (C3-C6) alkynyl , (Ci -C4) dialkyl, dialkyl, chloro or nitro mono-substituted to di-substituted benzene-23- This paper A degree is applicable to the Chinese National Standard (CNS) A4 ^ grid (210X297 mm) I:- ----- '—installed ------ order ----- f line (please read the precautions on the back before filling in this page) A7 B7 printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Indicate (α) group, or thienyl group; and R3 is hydrogen; (Ci _C4) alkyl group; (Ci _C4) haloalkyl group containing 1 to 3 halogen atoms; (Ci —C2) alkane group (C : -Cz) alkyl; propenyl which is unsubstituted or substituted with 1 to 3 halogen atoms; allyl; (C3-C6) alkyl; unsubstituted or substituted with 1 to 2 halogen atoms Propylmethyl; chloro- (C i -C2) alkyl; (Ci-〇2) alkanoylcarbonyl- (Ci_C2) alkyl; unsubstituted or substituted Element, methyl group, methyl group or containing 1 to 3 tooth atoms, phenyl group, nitro group or (Ct _C2) secondary group diamino substituted phenyl mono (Ci _C2) alkyl group, phenyl group may not be Substituted or mono-substituted to di-substituted with the same or different substituents; unsubstituted phenyl or thiophene; halogen, methyl, mesyl, halomethyl containing 1 to 3 halogen atoms, propyl Or nitro substituted or di-substituted phenyl; or unsubstituted pyridyl or halogen-containing methyl, methoxy, halomethyl containing 1 to 3 healthy atoms, cyano or Nitro mono- or di-substituted pyridyl; and X and Y are as defined in formula I. (23) The compound of formula I mentioned in (22), wherein: A is gas, R i is methyl,

Rz為甲基;未被取代的苯基或》立被鹵素,甲基, 甲氣基,三氟甲基或三氟甲氣基單取代到二取代的苯基; 和 R 3為甲基。 -24- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ^ 裝 訂 ( 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局—工消費合作杜印製 A7 B7 五、發明説明W ) (24) 式I化合物,其中: A 為 N C Η 3 , R X為甲基, R2為甲基;未被取代的苯基或_立被Α素,甲基, 甲氣基,三《甲基或三氰甲氧基單取代到二取代的苯基; 和 R3為甲基;未被取代的苯基或被俪自猜立被鹵素, 甲基,甲氣基,含1到3催鹵原子的鹵甲基,氱基或硝基 單取代或二取代的苯基;或未被取代的吡啶基或被値自播 立被鹵素,甲基,甲氣基,含1到3掴鹵原子的鹵甲基, 氰基或硝基單取代或二取代的吡啶基;而X和Y定義如式 I 〇 (25) 式I化合物,其中 X為氮原子; Y 為 0 R i X ;Rz is methyl; unsubstituted phenyl or monophenyl substituted by halogen, methyl, methy, trifluoromethyl or trifluoromethan to disubstituted phenyl; and R 3 is methyl. -24- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) ^ Binding (line (please read the precautions on the back before filling this page) Central Bureau of Standards of the Ministry of Economic Affairs-Industrial and Consumer Cooperation Du Printed A7 B7 5. Description of the invention W) (24) The compound of formula I, wherein: A is NC Η 3, RX is methyl, R2 is methyl; unsubstituted phenyl or thiol A, methyl, methyl gas Radicals, trimethyl or tricyanomethoxy mono-substituted to di-substituted phenyl; and R3 is methyl; unsubstituted phenyl or halogenated by methyl, methyl, methyl, containing Halomethyl of 1 to 3 halogen atom, mono- or di-substituted phenyl of propyl or nitro; or unsubstituted pyridyl or self-propagated halogen, methyl, methy, containing 1 Halomethyl to 3 slap halogen atoms, cyano or nitro mono- or di-substituted pyridyl groups; and X and Y are as defined in formula I 〇 (25) Formula I compounds, wherein X is a nitrogen atom; Y is 0 R i X;

Ri 1為(Ci 一 C4 )焼基;其中 A, Rt, R2和R3定義如式I。 (2 6) (25)所提到的化合物中·· A為氣原子; R i和R 2為甲基;Ri 1 is (Ci-C4) alkyl; wherein A, Rt, R2 and R3 are defined as in formula I. (26) (25) In the mentioned compounds, A is a gas atom; R i and R 2 are methyl;

Rs為氫;(C! -C4 )烷基;含1到3偏鹵原子 的(Ci _C4)豳烷基;(Ci -CZ)烷氣基一( Ci _C2 )烷基;未被取代或被1到3俪歯原子取代的 -25- 本紙張尺度適用中國國家標準(CNS ) A4^#· ( 210X297公釐) 丨;------{ I裝------訂-----f 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央橾準局貝工消費合作杜印装 A7 B7 五、發明説明(π) 丙烯基;烯丙基;(c3_ce)琢烷基;未被取代或被 1到2俪鹵原子取代的琢丙基甲基;氛基一 (Ci -C2 )烷基;(Ci _CZ )烷氣基羰基一 (Ci 一02 )烷 基;未被取代或被齒素,甲基,甲翥基或含1到3鶴β原 子,《基,硝基或(Ct — C2 )次烷基二氧基取代的苯 基一 (Ci _C2 )烷基,苯基可能未被取代或被相同或 不同取代基單取代到二取代;未被取代的苯基或被籲自猜 立被鹵素,甲基,甲氧基.含1到3雇鹵原子的鹵甲基, «基或硝基單取代或二取代的苯基;或未被取代的毗啶基 或被傾自玀立被鹵素,甲基,甲氣基,含1到3鹤鹵原子 的鹵甲基,氯基或硝基單取代或二取代的吡啶基。 (2 7) (26)所提到的式I化合物,其中: R3為氫;((:1一(:4)烷基或含1到3俪鹵原子 的(Cl —C4 )曲院基。 (28)式I化合物,其中 X為氮原子; Y 為 N ( R 1 2 ) R ! 3 ;Rs is hydrogen; (C! -C4) alkyl; (Ci _C4) alkyl containing 1 to 3 partial halogen atoms; (Ci -CZ) alkanoyl (Ci _C2) alkyl; unsubstituted or substituted 1 to 3 Atomic substitution of -25- This paper scale is applicable to Chinese National Standard (CNS) A4 ^ # · (210X297mm) 丨; ------ {I 装 ------ 定- --- f line (please read the precautions on the back before filling in this page) Ministry of Economic Affairs Central Bureau of Industry and Fisheries Consumer Cooperation Du Printing A7 B7 V. Description of Invention (π) Propylene; Allyl; (c3_ce) C-alkyl; C-propyl methyl unsubstituted or substituted by 1 to 2 halogen atoms; Amino- (Ci -C2) alkyl; (Ci _CZ) alkylcarbonyl- (Ci-02) alkyl ; Unsubstituted or substituted by dentyl, methyl, mesyl or containing 1 to 3 he β atoms, phenyl, nitro or (Ct — C2) hypoalkyldioxy substituted phenyl one (Ci _C2) Alkyl and phenyl groups may be unsubstituted or mono- to di-substituted with the same or different substituents; unsubstituted phenyl groups may be substituted by halogen, methyl or methoxy. Contains 1 to 3 halogens Atom halomethyl, «group or nitro mono- or di-substituted phenyl A substituted or unsubstituted piperidinyl or border Li Luo is poured from halogen, methyl, group A gas containing halomethyl 1 to 3 halogen atoms crane, chloro or nitro-substituted mono or di-substituted pyridyl. (2 7) The compound of formula I mentioned in (26), wherein: R3 is hydrogen; ((: 1-(: 4) alkyl or (Cl-C4) Quyuan group containing 1 to 3 halogen atoms). (28) The compound of formula I, wherein X is a nitrogen atom; Y is N (R 1 2) R! 3;

Ri 2和尺^ 3鎇自播立為氫或(Ci — C4 )烷基 ;其中A, Ri , Rz和R3如式I所定義。 (2 9) (28)所提到的式I化合物,其中: Y 為 NHz ,N (CH3 ) 2 或 NHCz Hs ; A為氣原子; R 1和R 2為甲基; *28&quot; 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I:------《 I裝------訂-----f 線 (請先聞讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印裝 A7 B7 五、發明説明(vl ) R3為氫;(Ci _C4 )烷基;含1到3鵃原子 的(Ci —C4 )鹵烷基;(Ci -Cz )烷氣基一( Ci-C2)烷基;未被取代或被1到3鵪曲原子取代的 丙烯基;烯丙基;(c3 _ce )環烷基;未被取代或被 1到2镳鹵原子取代的環丙基甲基;氱基一 (c , _C2 )烷基;(Ci —C2 )烷氣基羰基一 (Ci -c2 )院 基;未被取代或被豳素,甲基,甲氣基或含1到3艟鹵原 子,氰基,硝基或(Ci _c2 )次烷基二氣基取代的苯 基一 (Ci _CZ )烷基,苯基可能未被取代或被相间或 不同取代基單取代到二取代;未被取代的苯基或被催自猜 立被齒素•甲基,甲氧基,含1到3籲鹵原子的鹵甲基, 氱基或硝基單取代或二取代的苯基;或未被取代的毗啶基 或被個自獨立被鹵素,甲基,甲氧基,含1到3值鹵原子 的鹵甲基,氰基或硝基單取代或二取代的吡啶基。 (30) (29)所提到的化合物中: R3為氫;(Ci _C4 )烷基或含1到3镳鹵原子 的(Cl —C4 )幽院基。 (31) 式I化合物,其中X=C雙鍵為E形式。 式I化合物之製備如以下所述: (A)為了製得Y為N (Ri 2 ) Ri 3之式I化合物, Y為ORi i的式I化合物與HN (Ri z ) Ri 3反應 。該反應偽有利地於一惰性有機稀釋_中進行,例如在乙 酵之酵類,四氮呋喃之醚類,乙酗乙酯之酯類,二甲基亞 -27- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I ^ ^ I裝 訂 ( 線 (請先聞讀背面之注意事項再填寫本頁)Ri 2 and Chi ^ 3 are self-promoted as hydrogen or (Ci-C4) alkyl; where A, Ri, Rz and R3 are as defined in formula I. (2 9) The compound of formula I mentioned in (28), wherein: Y is NHz, N (CH3) 2 or NHCz Hs; A is a gas atom; R 1 and R 2 are methyl; * 28 &quot; Applicable to Chinese National Standard (CNS) A4 specification (210X297mm) I: ------ 《I installed ------ order ----- f line (please read the notes on the back before filling (This page) A7 B7 printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention (vl) R3 is hydrogen; (Ci _C4) alkyl; (Ci —C4) haloalkyl containing 1 to 3 atoms; ( Ci-Cz) Alkyl-mono (Ci-C2) alkyl; propenyl unsubstituted or substituted by 1 to 3 quaternary atoms; allyl; (c3_ce) cycloalkyl; unsubstituted or substituted by 1 Cyclopropylmethyl substituted with halogen atoms up to 2; tri- (c, _C2) alkyl; (Ci-C2) alkanoylcarbonyl- (Ci-c2) alkyl; unsubstituted or derivatized, Methyl, methyl group or containing 1 to 3 halogen atoms, cyano, nitro or (Ci _c2) hypoalkyl substituted phenyl mono (Ci _CZ) alkyl, phenyl may not be substituted or Mono- to di-substituted by interphase or different substituents; unsubstituted phenyl Prompted self-assured dentate • methyl, methoxy, halomethyl containing 1 to 3 halogen atoms, phenyl mono- or di-substituted phenyl or nitro; or unsubstituted pyridinyl Or it may be independently substituted by halogen, methyl, methoxy, halomethyl containing 1 to 3 halogen atoms, cyano or nitro mono- or di-substituted pyridyl. (30) Among the compounds mentioned in (29): R3 is hydrogen; (Ci _C4) alkyl or (Cl -C4) cryptic group containing 1 to 3 hydrogen atoms. (31) The compound of formula I, wherein the X = C double bond is in the E form. The preparation of the compound of formula I is as follows: (A) In order to prepare the compound of formula I with Y being N (Ri 2) Ri 3, the compound of formula I with Y being ORi i is reacted with HN (Ri z) Ri 3. This reaction is advantageously carried out in an inert organic dilution, for example, in the fermentation of ethyl yeast, the ethers of tetrazofuran, the ethyl esters of ethyl alcohol, dimethyl-27- This paper size is applicable to China Standard (CNS) A4 specification (210X297mm) I ^ ^ I binding (line (please read the precautions on the back before filling this page)

30486C A7 B7 五、發明説明(7 ) 碾之亞《類,二甲基甲醯胺之醯胺類或甲基異丁基之酮 類。甲基胺之使用形式可為氣體或溶解形式,例如在乙酵 中的溶液形式。方法之傳统進行湛度為0到401C,較佳 在室溫下。 (B)為了製得式I中之X, Y,八和111 —R3如式I 所定義(其中R3不為氳)的化合物,將一下式化合物30486C A7 B7 Fifth, the description of the invention (7) Grinding sub-class, dimethyl formamide amide or methyl isobutyl ketone. Methylamine can be used in gaseous or dissolved form, such as in solution in ethanol. The traditional method of performing the process is from 0 to 401C, preferably at room temperature. (B) In order to prepare the compounds of formula I X, Y, octa and 111-R3 as defined in formula I (where R3 is not radium),

R·: HONR ·: HON

A RiA Ri

其中A和R R3定義同上,與下式化合物反應 經濟部中央揉準局員工消費合作社印製Among them, A and R R3 are defined as above, and are reacted with the compound of the following formula.

其中X和Y定義同上,U為一離去基。 該反應為親核性取代反應,可在此類情況之傳統反應 條件下進行。離去基U較佳為氰,溴,碘,甲烷磺醏氯基 -2 8 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I^ I裝 訂 ^線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(7&gt; ) 或甲苯磺醯氣基。反應有利地在惰性有機稀繹_中,例如 環条醚類,例如四氫呋喃或二噁烷,酮類.例如丙酮,篇 胺類,例如二甲基甲醯胺,亞《類,例如二甲基亞《,及 在鹵如氫化納,硪酸納,磺酸錚,睡胺銪,三级胺,例如 三烷基胺,特別是二氮雜二環壬烷或二氮雜二環十一烷, 或氣化銀存在下,及在一 20*0和8 0¾之間的ffi度進行 ,較佳在Ot:到50t進行。 或者,該反應可以與相轉移觸媒在有機溶剤如氯化次 甲基及在鐮性水溶液,如氳氧化銷溶液,及相轉移觸媒如 硫酸篇四丁基銨存在下在室溫下進行。 所得到的式I化合物可被習知方法加以分離和鈍化。 換言之,所得到的異構物混合物,例如E/Z異構物混合 物可被習知方法加以分離,得到鈍異構物,例如Μ色層分 析或分皤结晶。 作為起始物質的通式II的肟為習知的,或者可由習 知方法加以製備(J· Che·. Soc., Perkin Trans II 537 ( 1990) ; Ber. Deutsch. Che·. Ges. 62 , 866 ( 1929); Gazz. Chi·. Ital. 37 II, 147 (1907); Liebigs Ann. Che·· 262, 305 (1891)〇 換言之,式I I I的起始物質可由習知方法加以製備 ,例如 European Patent Publication EP-A-203 6 0 6 (BASF)及其中所引述文獻或者Angei». Che·. 7 1 , 3 4 9- 3 6 5 ( 1 95 9)所述者。 -29- 本紙張尺度適用中國國家標準(CNS ) A4規格(2丨0X297公釐) — 1------入 —裝------訂-----{線 (請先閲讀背面之注意事項再填寫本頁) ^〇486〇 A7 _________B7五、發明説明(W ) (C)為了製備式I中之a為氡,X, γ和r 式I所定義的化合物: 一下式化合物 R 3如X and Y are as defined above, and U is a leaving group. This reaction is a nucleophilic substitution reaction and can be carried out under conventional reaction conditions in such cases. The leaving group U is preferably cyanogen, bromine, iodine, methanesulfonyl chloride-2 8-This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) I ^ I binding ^ line (please read the back first Note: Please fill out this page) A7 B7 printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of invention (7 &gt;) or tosylate. The reaction is advantageously in an inert organic diluent, such as cyclic ethers, such as tetrahydrofuran or dioxane, ketones. For example, acetone, amines, such as dimethylformamide, sub-class, such as dimethyl Sub- ", and in halogen such as sodium hydride, sodium sulfate, beryllium sulfonate, europium, tertiary amine, such as trialkylamine, especially diazabicyclononane or diazabicycloundecane , Or in the presence of vaporized silver, and a ffi degree between 20 * 0 and 8 0¾, preferably from Ot: to 50t. Alternatively, the reaction can be carried out at room temperature with a phase transfer catalyst in the presence of an organic solvent such as methine chloride and in a sickle aqueous solution, such as an oxirane solution, and a phase transfer catalyst such as tetrabutylammonium sulfate. . The resulting compound of formula I can be isolated and passivated by conventional methods. In other words, the resulting isomer mixture, for example, the E / Z isomer mixture, can be separated by a conventional method to obtain a passive isomer, such as M-chromatographic analysis or crystallization. The oximes of the general formula II as starting materials are known or can be prepared by conventional methods (J · Che ·. Soc., Perkin Trans II 537 (1990); Ber. Deutsch. Che ·. Ges. 62, 866 (1929); Gazz. Chi .. Ital. 37 II, 147 (1907); Liebigs Ann. Che. 262, 305 (1891). In other words, the starting material of formula III can be prepared by conventional methods, such as European Patent Publication EP-A-203 6 0 6 (BASF) and the documents cited therein or those described in Angeli ». Che .. 7 1, 3 4 9- 3 6 5 (1 95 9). -29- The size of this paper Applicable to China National Standard (CNS) A4 specification (2 丨 0X297mm) — 1 ------ Into—install ------ order ----- {line (please read the precautions on the back first (Fill in this page) ^ 〇486〇A7 _________B7 V. Description of the invention (W) (C) In order to prepare the compound of formula I where a is radon, X, γ and r The compound defined by formula I:

0H0H

IV 經濟部中央樣準局員工消費合作社印製 其中X· Y, Ri和1?2定義同上,舆下式化合物反應 u - R 3 V R3定義同式I , U定義同式I I I (R3既不是氫,也 不是苯基或ftt淀基)。 此反應為如(B)所述的親核性取代反應。 (D)為了製備式IV中X, Y, R!和只2如式1所定 義的化合物,進行以下的程序: 一下式化合物 〇IV. Printed by the Employees Consumer Cooperative of the Central Bureau of Samples of the Ministry of Economics where X · Y, Ri and 1? 2 have the same definition as above, and the following compounds react u-R 3 V R3 has the same definition as Formula I and U has the same definition as Formula III (R3 is neither Hydrogen, nor phenyl or ftt). This reaction is a nucleophilic substitution reaction as described in (B). (D) In order to prepare X, Y, R! In Formula IV and only 2 compounds as defined in Formula 1, the following procedure is carried out: The compound of formula 〇

VI I : 人 —裝 —訂 一線 (請先閲讀背面之注意事項再填寫本頁) 30- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央標準局員工消費合作社印製VI I : Person-installation-order line (please read the precautions on the back before filling in this page) 30- This paper size is applicable to China National Standard (CNS) A4 specification (210X297mm) Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs system

A7 _B7 五、發明説明(π) 其中X, Y, Ri和只2同上所定義.輿羥基胺或其《如 氫氰化物反應。此反鼷有利地以吡啶或甲酵作為溶劑,在 -201C和+ 80¾之間,或者在甲酵沸點,較佳在Ot: 到5 Ot之間反應,若使用甲醇則必須用_,例如用_(金 屬碩酸鹽,例如硪酸鉀,三级胺,例如三乙基胺或二氮雜 二環壬烷,吡啶或氣化銀。 用類似(B)所述方法製備式VI的酮。式VI的嗣 和其製備方法被敘述於,例如EP- 3 7 - 6 2 9 , EP- 5 0 6 14 9 , EP-403 618, EP-414 513, EP-463 488, EP-472 300, EP-4 6 0 5 7 5 , W0- 9 2/ 184 94 及其它刊物。 (E)為了製備式I中A, X, 丫和!^^ — R3如式I定 義,但R3不為氫之化合物,進行以下的程序,例如 一下式化合物A7 _B7 V. Description of the invention (π) where X, Y, Ri and only 2 are as defined above. Hydroxylamine or its reaction such as hydrocyanide. This reaction is beneficial to use pyridine or formazan as the solvent, between -201C and + 80¾, or at the boiling point of formazan, preferably between Ot: to 5 Ot, if you use methanol, you must use _, for example with _ (Metal master salt, such as potassium silicate, tertiary amine, such as triethylamine or diazabicyclononane, pyridine or silver vapor. The ketone of formula VI is prepared in a manner similar to that described in (B). Formula VI and its preparation method are described in, for example, EP-3 7-6 2 9, EP-5 0 6 14 9, EP-403 618, EP-414 513, EP-463 488, EP-472 300, EP-4 6 0 5 7 5, W0-9 2/184 94 and other publications. (E) In order to prepare A, X, Y and Y in formula I! ^^ — R3 is as defined in formula I, but R3 is not hydrogen Compounds, perform the following procedure, for example

&quot;A\d VII N R3 其中A, X, 丫和只^ _R3如上定義,與甲基化試_例 如甲基礮,二甲基硫酸鹽或二重氰甲烷反謳。此反應有利 -31- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 丨;------{ —裝------訂-----{線 (請先閲讀背面之注意事項再填寫本頁) S〇486〇 A7 B7 i、發明説明(“) 地在_如磺酸押或氫化銷存在下於合適溶_和合適反應湛 度下進行(例如參考H.S. Ankerund H.T. Clarke; Organi Synthesis, Coll. 3, 172)。 (F)為了製備式VI I中A, X, Y和Ri _R3定義 同式I的化合物,有利地進行以下程序: 一下式化合物 Λ,&quot; A \ d VII N R3 where A, X, Y and ^ _R3 are as defined above, and methylation test _ such as methyl acetate, dimethyl sulfate or dicyanomethane reaction. This reaction is favorable -31- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) 丨; ------ {— 装 ------ 定 ----- {线 (PLEASE Read the precautions on the back before filling in this page) S〇486〇A7 B7 i. The description of the invention (“) is carried out in the presence of sulfonic acid or hydrogenated pins in a suitable solution and a suitable reaction degree (for example HS Ankerund HT Clarke; Organi Synthesis, Coll. 3, 172). (F) In order to prepare compounds of formula I where A, X, Y and Ri_R3 define the same formula I, it is advantageous to carry out the following procedure:

A vm 經濟部中央標準局貝工消費合作社印製 其中A, Y和Ri _R3定義同上,在鐮存在下採用類似 於EP-A-178 826所述方法與甲酸鹽反鼴,或者與亞硝酸進 行硝化反應,或者在鹹存在下採用類似於EP-A- 254 426所 述方法舆腈反應。 另一種合成式VII化合物的可能方式為以下的反* 一下式化合物 0A vm Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy where A, Y and Ri _R3 are defined as above. In the presence of sickle, a method similar to that described in EP-A-178 826 is used to react with formate, or with nitrous acid Carry out a nitration reaction, or use a method similar to that described in EP-A-254 426 and a nitrile reaction in the presence of saltiness. Another possible way to synthesize the compound of formula VII is the following trans * compound of formula 0

AA

IX IJ-------ί I裝------訂-----f 線 (請先閱讀背面之注意事項再填寫本頁) 32- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央標準局員工消費合作社印装 A7 B7 五、發明説明(Μ ) 其中A, Y和Rt到只3定義同上,採用類似EP-A-178 8 2 6所述方法與甲氣基次甲基三苯基磷?反應,或者採用 類似 EP-A- 2 54 4 2 6所述方法與氣一甲基羥基胺(或其鹽 )反應。 本發明也提供新穎的式VI I, VI I I和IX化合 物。 目前已經發現式I化合物具備控制植供致病微生物的 殺微生物性質,特別是徽皤,也是最符合實際需要的。該 化合物具備非常有利的治療、預防和,待別是条统性質, 可被用於保護大量農作植物。使用式I的活性成份,各種 在有用植物的作物之檀物或部份植物(果資.花,葉,莖 ,結節,根)所發現的害典可被破壤,甚至可以處理在無 植物致病撇生物時間稍後所形成的植物部份。 式I化合物可進一步作為處理種子的種子(果實,结 節,種子)敷料試以及保議不受徽齠戚染和抗土壤植 物致病徽菌的幼苗植物。 式I化合物對以下植物致病性徽豳具活性,例如徽鹧 inperfecti(特別是蠶徽菌颶,更包括Pyricularia, Helninthosporiun, 梭徽菌, S e p t o r i a ,皮疼徽酺 ,Cercosporella和 Alternaria);擔子 03 屬(例如根瘤菌, Henileia, Puccinia);囊子聞鼷(例如 Venturis 和IX IJ ------- ί I installed ------ order ----- f line (please read the precautions on the back before filling in this page) 32- This paper size is applicable to China National Standards (CNS ) A4 specification (210X297 mm) A7 B7 printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of invention (Μ) Among which A, Y and Rt up to only 3 are defined as above, similar to EP-A-178 8 2 6 What is the method described with trimethylphosphine? Reaction, or using a method similar to that described in EP-A-2 54 4 2 6 with gas monomethylhydroxylamine (or its salt). The invention also provides novel compounds of formula VI I, VI I I and IX. It has been found that compounds of formula I possess microbicidal properties for controlling plant-providing pathogenic microorganisms, especially Anhui, which is also the most in line with actual needs. The compound has very favorable therapeutic, preventive and, in general, general properties, and can be used to protect a large number of agricultural plants. Using the active ingredients of formula I, all kinds of sandalwood found in crops of useful plants or some plants (fruits, flowers, leaves, stems, nodules, roots) can be broken through the soil, and can even be processed in the absence of plants. The pathogenic part of the plant formed later in the biological time. The compound of formula I can be further used as a seed dressing test for the treatment of seeds (fruit, nodules, seeds) and seedling plants that are protected from the infection of the Anhui strain and resistant to the pathogenic microorganisms of soil plants. Compounds of formula I are active against the following plant pathogenic emblems, such as partridge inperfecti (especially H. punctatus, also including Pyricularia, Helninthosporiun, Clostridium spp., S eptoria, dermatoglyphics, Cercosporella and Alternaria); 03 genus (eg, Rhizobium, Henileia, Puccinia); sac smelling (eg Venturis and

Erysiphe,Podosphaera,串珠發羼,Uncinula);0〇Bycetes( -33- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 丨:------' I裝------訂-----^線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作杜印製 A7 B7 五、發明説明(β) 例如 Phytophthora, Peronospora, B r e i a , Py t h i u·, Plasoopara)〇 式I化合物也是對抗經常出現於有用植物和農業及圃 蕕之裝飾昆典和恙巖的有用活性成份,特別是在稻米,柿 花,蔬菜和水果,以及森林,同時溫血品種,魚和植物對 其具有較佳的相容性。式I化合物待別適合用於控制穀作 物,水果和蔬菜的昆鑫,特別是控制會破壤植物的昆巔。 。本發明的活性成份可應用的其它領域為保護键存貨物和 材料,以及術生保健匾域,待別是保護家餐動物和事生産 生畜。式I化合物一般敏烕但也具有抗性的寄鑫的所有或 掴別成長階段都具有活性。其活性活性可能變得明顯,例 如立刻或只在經過某段時間(例如在蛻變期閭)之後破壤 害螽或是減少産卵和/或孵出速率。 以上所述害鑫實例為來自鱗翅目者,例如播葉蛾鼷, 小捲葉蛾羼,透翅蛾靨,地老虎羼,阿拉巴馬argillaceae ,aaylois屬,黎豆夜蛾颶,捲葉蛾篇,播藥羼,紋夜娥, busseola,粉斑蝗,捲葉蛾屬,chiloJR,捲葉蛾羼,葡萄 果蠢蛾,设捲螟羼,播葉蛾JR, cochylisJK,鞘蛾羼, crocidoloDia binotalis, Cryptophe lebia leucotreta ,Cyd ia屬,玉米螟· Diparops is castanea ,缔紫實蠱屬 ,斑蝗蛾靥,黃螟羼.Eupoecilia aabiguella.茶籌娥屬 ,切根矗靨,小捲蛾臑,嫌小捲蛾,撺鈴蠱羼,菜螟,美 圃白蛾,番茄蠢娥,旋蛾潛蛾,細蛾鼷,藥典,毒蠘颺, -34- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I;------气 —裝------訂-----^線 (請先閣讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 304860 A7 __B7___ 五、發明説明(θ ) ®ll蛾羼,天幕毛典羼,甘豔夜蛾,烟草天蛾,尺蠛騰, 玉米螟,播葉鋸蜂屬,捲蕖蛾羼,捲蕖蛾,红鈐蠱, 馬#薯塊莖蛾,菜粉蝶屬,小菜蛾,m蛾羼,白螟屬,夜 蛾羼,捲藥蛾屬,粉纹夜娥和嚴蛾羼; 鞘翅沫蜂目者,例如叩甲颺,象甲屬,黏龕,甜菜脛 期ί甲,世界臑,象甲羼,皮蠢羼,瓜葉甲羼,鼷巖羼,潛 娥羼,馬鈴薯甲鑫,象甲属,思金龜羼,尾蜂羼,象甲羼 ,小蠢饜,麗金龜靥,跳甲屬,根谋靨,金龜,谷象羼, 麥蛾屬,粉甲屬,擬谷盗屬和斑皮蠢羼; 直翅目者,例如非蠊羼,小蠊,蠼蛄羼,馬得拉蜚娜 •飛煌屬,大蠊颶和炸蜢羼; 等翅目者,例如白蟻羼; 哦蟲目者,例如象害虱屬; 虱目者,例如Haeaatopinus屬和長顎虱屬,多虱羼, 纓綿蚜羼和根瘤蚜颺; 食毛目者,例如Daaelinea颶和羽虱靨; 纓翅目者,例如薊馬鼷,薊馬羼,嫌黼馬羼,榇蓟馬 羼,棉薊馬羼和橙薊馬; 異翅目者,例如葉蜂靥,Distant ie 1 la theobroia , 红春展,Euchistus屬,盾春JR,錄春屬,錄春JK,期春屬 ,R h 〇 d n i u s 靥,S a h 1 b e r g e 11 a s i n g u 1 a r i s,稻春羼和玀春 羼; 同翅目者,例如棉粉虱,粉虱,圔紅蚧羼,蚜科,蚜 -35- 本紙張尺度適用中國國家揉準(CNS ) A4規格(2丨0X297公釐) 丨:------〈I裝------訂-----f 線 (請先聞讀背面之注意事項再填寫本頁) 經濟部中央橾準局員工消費合作社印製 A7 B7 五、發明説明(3。) 羼,(蚧屬,梅粉虱,蟠蚧羼,茶褐圃蚧,蕃薇輪蚧,褐 軟蚧,葉蟬羼,蘋棉蚜,斑蕖蟬,GascardU鼷,飛虱屬, 李蠼蚧,緬蚧羼,長管蚜颺,瘤額蚜羼,蕖蜂羼,稻虱屬 ,天牛屬,續棉蚜羼,粉蚧屬,白蚧羼,粉蚧羼,木虱颺 ,桃棉蚧,果國蚧属,鎰管蚜羼,盔蚧屬,葉蜂屬,二叉 蚜屬,吸漿鑫羼,溫室白粉虱,木虱和橘盾蚧; 膜翅目者,例如葉蜂,Attas羼,麥莖蜂屬,鋸角藥蜂 羼,鋸角葉蜂,葉蜂羼,田蟻簏,廚蟻,鋸角蕖鲦羼,火 蟻属和胡蜂颺; 雙翅目者,例如伊蚊羼,Anther igona soccata,毛 蚊,红頭麗蠼,實蠼屬,輪蚧颺,库纹鼷,疽蠅鼷,實繩 鼷,黃猩猩果蠅,既蠅,大枯葉娥属,舌蠅屬,皮孅饜, 象甲屬,潛蠼屬,綠蠼屬,潛蠼属,家蠅JR, #蠼驊,角 蚜屬,麥捍蟝,甜菜潛葉蠼,蚤蠼屬,蘋果蠅,輦蚊屬, 螫蠅屬,牛虻羼,夜蟬羼和大蚊颶; 蚤目者,例如葉蚤羼和東方鼠蚤雙尾目者,例如西洋 衣魚; 蜱滿目者,例如粗脚粉滿,拮芽觼滿,蘋刺觼满,花 婢羼,隠喙蜱羼,小牛蜱靥,短須谋颶,苔滿, Calipitriaecus spp.,癢滿JH,雜皮剌满,鷄耳瀝東方藥 钂,隳谋 JK , Hyaloaia spp .,硬婢屬.0 lygonycbus pratensis, 嗛姆 JR .紅爪谋 81,P h y 11 o c o p t r u t a oleivora, 倒多食趺線谋,觸滿羼, 扇頭蜱JK ,根滿靥 -3 6 * 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公嫠) 丨一------/丨裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央梯準局貝工消費合作社印裝 * A7 __B7 五、發明説明(3&gt;丨) ,疥滿羼,趺線滿羼和藥滿羼。 合適作為目標的典作物為,特別是,穀類,如麥,大 麥,裸麥,燕麥,米,玉米或高梁*甜菜類,如甜菜或草 料甜菜;水果,如梨果,核果和軟果,如蘋果,梨,李子 ,桃子,杏仁,櫻欲或莓,如草莓,醭莓或黑莓;豆科植 物·例如豆,馬尾藻,豌豆或大豆;油農作物,例如油菜 籽,芥末,罌粟,橄欖,向日癸,椰子,蓖爾油,可可, 或苒花生;葫蘆類,例如南瓜,胡瓜或西瓜;纖維植物, 例如綿,亞麻,大麻或黃麻;柑橘類植物,例如橘子,檸 樺,蒱萄柚或橘柑;蔬菜,例如菠菜,萵苣,蘆荀,甘藍 ,胡繾葡,葸,蕃伽,馬鈴譬,或胡椒;Lauraceae,例如 咢梨,肉桂或樟腦;和烟草,果核,咖琲,茄子,甘蔗, 茶,胡椒,葡萄,蛇麻草,乳臞植物和裝嫌性植物。 I化合物的組成物活性包括藉着添加其它殺龕劑和/ 或殺恙蟲劑而使其能夠被實質地擴展並配合各種琿境的使 用。合適的添加代表如以下各類的活性成份:有機磷化合 物,硝基酚和其衍生物,甲釆,脲,氨基甲_酯,除蠱菊 ,氰化烴和捍ilthuringiensis製備物。 循往例,式I活性成份像以組成物形式被使用,可同 或間歃式與其它活性成份一起被施用於某®域或植物上。 這些其它活性成份可包括肥料,微量元素介臁或其它會影 镰植物生長的製備物。趣擇性的除萆劑和殺典劑,殺徽豳 劑,殺菌劑,殺線蠱劑,殺軟鼸動物薄或逭些製備物的混 -37- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) &quot; 丨^ { I裝------訂-----f 線 (請先聞讀背面之注意事項再填寫本頁) ^〇486〇 a7 B7 五、發明説明(Si) 合物,可含或不含其它配方技《傅統載龌,界面活性_或 其它增強效用添加劑。 合鏟的載體和添加_可為固黼或液黼,是此配方技藝 中常用的物質,例如天然或再生礦物質,溶分散 潤濕剤,增粘结合_或肥料。 以下為合適的溶两:芳香条烴,較佳為C8到匚^ 2 者,例如二甲苯混合物或取代莱,肽酸,例如二丁基肽 酸鹽或二辛基酞酸鹽,脂肪条熳,例如琛己烷或石蠟,酵 類和二酵類以及其_和酯,例如乙酵,乙二酵,乙二酵單 甲基醚或乙基醚,酮,例如環己麵,強極性溶劑.例如N 一甲基—2 —吡咯烷酮,二甲基亞《或二甲基甲醯胺,和 未琛氣化或環化植物油,例如琢氣化椰子油或大豆油;或 水。 常用作為灰和可分散粉末的固鳢載體例如為磨碎天然 岩石,例如方解石,滑石,高嶺土,脱蒙土或attapuUite 〇 經濟部中央樣準局員工消費合作社印製 (請先閲讀背面之注意事項再填寫本頁) 可大大降低應速率的待別有利的增強添加劑為天然( 動物或植物)或合成磷脂(來自腦磷脂和卵磷脂条列&gt; , 其可得自於,例如大豆。 依所調配式I活性成份的性質而定,合適的界面活性 «[化合物為非雄子,»雄子和/或陰離子界面活性朗,其 具傭優良乳化性,分散性和級湎性質。醮該理解的是界面 活性黼也代表界面活性_混合物。 -38- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央揉準局負工消費合作社印製 A7 B7 五、發明説明(β ) 合適的陰雄子界面活性剤可被稱為水溶性鹽,也可被 稱為水溶性合成界面活性化合物。 皂為金羼鹽,鹼土金展鹽或取代或未取代高硪數脂肪 酸(Ci 〇 — C2 2 )的銨鹽,例如油酸或硬脂酸的納麵 或鉀*,或脂肪酸天然混合物的納鹽或押鹽,其可得自於 ,例如椰子油或妥爾油。可一提的尚有脂肪酸甲基牛磺酸 鹽。 合適的非離子界面活性爾主要為脂肪条或琛勝肪条酵, 飽和或不飽和脂肪酸和烷基酚的聚二酵醚衍生物,其(脂 肪条)自由基可含有3到30艏二酵醚基和8到20«磺 原子以及烷基酚的烷基自由基中含6到18鐮磺原子。 非離子界面活性«的資例包括壬基酚聚乙氣基乙酵, 蓖麻油聚二酵醚,聚氣化丙烯/聚氣化乙烯加成物,三丁 基苯氣基聚乙氣基乙酵,聚乙二酵和辛基苯氣基聚乙氣基 乙酵。 其它合適的物質為聚氣乙烯山梨耱酵齋的脂肪酸 例如聚氣基乙烯山梨耱酵酐三油酸酯。 __子界面活性主要為季銨,其含有至少一種8到 22镇磺原子的烷基自由基作為取代基,其具備低鈒曲化 或自由魈烷基,苄基或低级羥基烷基自由基,作為進一步 的取代基。該》較佳以鹵化物,甲基硫酸·或乙基硫酸鹽 形式存在,例如硬脂醒基三甲基氰化銨或苄基二(2 —氛 乙基)溴化銨。 -39- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 丨:------丨裝------訂-----^線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局貝工消費合作社印製 A7 _ B7 五、發明説明 照往例,農化製備物包括Ο.1到99%,特別是0 .1到95%的式I活性成份.99. 9%到1%,特別 是99. 9到5%固讎或液醱添加用和0到25%,待別 是0.1到25%界面活性雨。 雖然商品較佳使用濃缠組成物,终端消簧者可循往例 地使用稀釋组成物。 組成物也可以包括其它添加爾,例如安定爾,消泡_ ,粘度讕整劑.结合劑,增粘_,肥料或其它活性成份供 特殊用途。 配方,也就是組成物,裂備物或混合物,其包括式I 活性成份及有或無固醴或液體添加劑,像製備於習知方法 ,例如擻底混合和/或研磨活性成份輿延展»,例如溶劑 (混合物),固體載體,及適當地,界面活性化合钧(界 面活性劑)。 在保護農作物領域的一較佳鼴用方法是在植物樹蕖( 樹葉應用)上,其使頻率和速率依受特別害典烕染的危險 程度而定。然而,活性成份也可以經由根部糸统(条统作 用)抵達植物,其像藉著液體組成物将植物所在地灞潤或 著將固釀形態的活性成份加入植物所在地,例如加入土壤 中,例如以顆粒形式(土壤應用)。在水稻方面,此種顆 粒可被計量加入滿水的水稻田。或者,式I化合物可用浸 漬核果於液钃組成物或用一固體組成物塗佈方式投予種子 核果(塗佈)。原則上,使用式I化合物可保護任何型態 -4 0- 本&amp;張尺度適用中國國家標準(€灿)八4規格(210父297公釐) IJ-------ί I裝------訂-----線 (請先閲讀背面之注意事項再填寫本頁) Α7 Β7 五、發明説明(κ) 的植物繁殖材料。 式I化合物被作為純活性成份或最好是與此技藝配方 所常用的輔助剤一起使用,然後依已知方式予以加工,得 到例如可乳化濃縮物,直接可噴式或可稀释溶液,稀釋乳 化液,可濕潤粉末,可溶粉末,粉塵和顆粒,也有含於聚 合物質的膠囊。應用方法舉凡噴塗,噴霧,塗粉,分散或 澆注以及組成物均被灌定以符合目的和一般琛境禰要。較 佳的施予速率循往例為1克到2公斤的活性成份/銪,較 佳25克到800克活性成份/畝,特佳為50克到40 〇克活性成份/畝。作為種子敷料産物時,每公斤種子使 用量較佳為0. 001克到1. 0克活性成份。 以下的賨例旨在更詳细的説明本發明,並不對本發明 造成任何限制。 製備實例 賁例Η _ 1 : 製備 IJ------成—裝------訂-----{' 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製Erysiphe, Podosphaera, Beaded Hair Uncinula); 0〇Bycetes (-33- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 丨: ------ 'I installed ---- --Subscribe ----- ^ Line (please read the precautions on the back before filling in this page) A7 B7 printed by the consumer cooperation of the Central Standards Bureau of the Ministry of Economic Affairs V. Invention Instructions (β) For example Phytophthora, Peronospora, Breia , Py thiu ·, Plasoopara) 〇The compound of formula I is also a useful active ingredient against Kun Dian and Chi Yan often appear in useful plants and agriculture and garden decoration, especially in rice, persimmon, vegetables and fruits, and forests, At the same time, warm-blooded varieties, fish and plants have better compatibility. The compound of formula I is suitable for controlling Kunxin, cereals, fruits and vegetables, especially Kunding, which can control soil-breaking plants. . Other fields in which the active ingredients of the present invention can be applied are the protection of key-stored goods and materials, as well as the field of health-care plaques, except for the protection of domestic animals and production of live animals. Compounds of formula I are generally sensitive but also resistant to all stages or stages of growth. Its active activity may become apparent, for example, breaking the soil immediately or only after a certain period of time (for example, during the metamorphosis period), harming the borer, or reducing the rate of spawning and / or hatching. Examples of the above-mentioned pests are from Lepidoptera, such as leaf moth reeds, small leaf moth reeds, winged moth deer, ground tiger reeds, Alabama argillaceae, aaylois genus, Trichosperma spp., Leaf moth articles, seed medicine羼, 繼 夜 娥, busseola, powder spotted locust, leaf moth genus, chiloJR, leaf leaf worm moth, grape fruit stupid moth, snail moth roll, leaf moth JR, cochylisJK, sheath moth roll, crocidoloDia binotalis, Cryptophe lebia leucotreta, Cyd ia Genus, corn borer · Diparops is castanea, Associated purple chrysanthemum, locust moth moth, yellow moth. Eupoecilia aabiguella. Tea genus, cut root root moth, small roll moth, suspected small roll moth, ringworm grub Kei, cabbage borer, Meipu white moth, tomato stupid, spiny moth latent moth, fine moth reed, pharmacopoeia, poisonous beetle, -34- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) I; ------ Air-installed ------ Ordered ----- ^ line (please read the precautions on the back first and then fill in this page) Printed 304860 A7 __B7___ by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs V. Description of the Invention (θ) ®ll mothweed, Tianmu Maodiange, Spodoptera exigua, tobacco hawkmoth Inchworms, corn borers, sawdust beetles, leafworm moths, leafworm moths, red chrysanthemum, horse # potato tuber moth, cabbage butterfly, diamondback moth, diamondback moth, mothworm, white borer, noctuid , Coprinus spp., Eriocheirium spp., And Yange 羼; Coleoptera moth bees, such as percussion yang, weevil, stick niche, beet tibia, world jellyfish, weevil stalk, skin stupid 羼, Cucurbita repens, Yan Yan, Qian'e Yi, Potato Jiaxin, Weevil, Sichatou, Tail Bee, Weevil, Little Stupid, Lachatina, Lepidoptera, Genmous, Scarab , Gu Xiang Ke, wheat moth genus, pink genus, Pseudospirulina genus, and Dermatoglyphus; Orthoptera, such as non-Cockroaches, cockroach, 蠼 辄 羼, Madeira Cna • Feihuang, Periplaneta and fried cockroaches; Isoptera, such as termite knots; Oh, insects, such as the genus Pseudomonas spp; lice eyes, such as the genus Haeaatopinus and the long jaw lice, polyphasic knot, Aphis gossypii, and Rhizobium aphid; Trituroptera, such as Daaelinea hurricane and feather louse; Thysanoptera, such as Thrips, Thrips, Thrips, Thrips, Thrips and Thrips; Heterowing For example, the leaf beetle, Distant ie 1 la theobroia, Red Spring Show, Eustusus, Dunchun JR, Spring Recording, Spring Recording JK, Spring Spring, R h 〇dnius Tall, S ah 1 berge 11 asingu 1 aris , Dao Chun Yi and Lu Chun Yi; Homoptera, such as cotton whitefly, whitefly, stag beetle, aphididae, aphid-35- This paper scale is applicable to China National Standard (CNS) A4 specifications (2 丨0X297mm) 丨: ------ <I installed ------ ordered ----- f line (please read the precautions on the back and then fill out this page) Staff of the Central Bureau of the Ministry of Economic Affairs A7 B7 printed by consumer cooperatives V. Description of invention (3. ) 羼, (coccidioides, Paleididae, Pseudococcidae, Pseudococcinea spp., Pterocarya spp., Pseudococcidae, Leafhopper, Phyllostachys aegypti, Spotted hopper, GascardU spp., Plant genus, Pseudococcidae, Burmese coccinea, long-tube aphids, tuft-fronted aphid, echidium, ricehopper, genus Cerambycidae, continuous cotton aphids, mealybugs, white scaleworms, mealybugs, wood louse, peach cotton scales , Coccinella spp., Ytterbium aphid, Helmetidae, Leaf beetle, Aphid spp., Syrup Xingong, Greenhouse powdery mildew, Psyllium, and Orange shield scale; Hymenoptera, such as leaf wasps, Attas羼, wheat stalk bee, sawhorn medicine bee horn, saw horn bee, leaf bee horn, field ant gui, kitchen ants, saw horned minnow, fire ant genus and wasp larvae; diptera, such as Aedes Kei, Anther igona soccata, Mosquito mosquito, Red-headed lizard, Pterocephalus spp., Coccinella spp., Cucurbita ruficollis, Nematode falcon, Rope reed, Chimpanzee Drosophila, Both flies, Erythris spp., Glossa , Leather skin, weevil, latent genus, green genus, latent genus, Musca domestica JR, # 蠼 骅, horn aphid, wheat flies, beet leaf larvae, flea genus, apple flies, yam Mosquito, sting fly, gadfly, night cicada and Mosquito hurricanes; Flea-orders, such as leaf flea and Diptera, such as Western fishes; Tick-eyes, such as thick-footed powder, budding buds, apple spines, flowering worms, beaks Tick, calf tick, hurricane, moss covered, Calipitriaecus spp., Itch full JH, miscellaneous skin full, chicken ear leached oriental medicine spp., Yuanmou JK, Hyaloaia spp., Hard genus. 0 lygonycbus pratensis, 嗛 姆 JR. Red Claw 81, P hy 11 ocoptruta oleivora, Inverted multi-eating squirrel, Manchuria, Fan tick Tick JK, Root Manchu-3-3 * This paper size is applicable to China National Standard (CNS) A4 specification (210X297 gong mai) 丨 一 ------ / 丨 installation ------ order ----- f line (please read the precautions on the back first and then fill out this page) Central Ministry of Economic Affairs Printed by Jubei Consumer Cooperatives * A7 __B7 V. Description of the invention (3> 丨), Shimangong, Fuxianmang and Yaomang. Typical crops suitable as targets are, in particular, cereals such as wheat and barley , Rye, oats, rice, corn or sorghum * beets such as beets or forage beets; fruits such as pears, stone fruits and soft fruits such as apples, pears, Plums, peaches, almonds, cherry blossoms or berries, such as strawberries, raspberries, or blackberries; legumes such as beans, sargasso, peas, or soybeans; oil crops, such as rapeseed, mustard, poppy, olive, Xiangri, Coconut, castor oil, cocoa, or peanuts; cucurbits, such as pumpkin, courgette, or watermelon; fibrous plants, such as cotton, flax, hemp, or jute; citrus plants, such as orange, lime birch, konjac, or tangerine ; Vegetables, such as spinach, lettuce, reeds, cabbage, cabbage, rice, fanga, mala, or pepper; Lauraceae, such as pear, cinnamon, or camphor; and tobacco, pits, kana, eggplant, Sugar cane, tea, pepper, grapes, hops, milkweed plants and suspicion plants. The compositional activity of the I compound includes the ability to be substantially expanded by the addition of other niche and / or tsutsugamushi and to be used in a variety of fields. Suitable additions represent the following types of active ingredients: organophosphorus compounds, nitrophenols and their derivatives, formazan, urea, carbamate, pyrethrum, cyanogenated hydrocarbons and ilthuringiensis preparations. Conventionally, the active ingredient of formula I is used as a composition, and it can be applied to a certain field or plant together with other active ingredients in the same or intermittent form. These other active ingredients may include fertilizers, trace elements, or other preparations that affect the growth of sickle plants. Interesting demixing agents and antidote agents, antimicrobial agents, fungicides, thread killing agents, soft killing animal thinners or a mixture of these preparations-37- This paper scale is applicable to China National Standards (CNS) A4 specifications (210X297mm) &quot; 丨 ^ {I installed ------ ordered ----- f line (please read the precautions on the back before filling this page) ^ 〇486〇a7 B7 5. Description of the invention (Si) compound, may or may not contain other formulation techniques "Fu Tong Zai Qiang, interface activity_ or other enhancement effect additives. Carriers and additives for shoveling can be solid or liquid. They are commonly used in this formulation technique, such as natural or regenerated minerals, dissolving, dispersing, wetting, and thickening bonding_ or fertilizers. The following are suitable solvents: aromatic hydrocarbons, preferably C8 to ^ 2, such as xylene mixtures or substituted Lei, peptidic acid, such as dibutyl peptidate or dioctyl phthalate, fatty strips , Such as hexane or paraffin, enzymes and second enzymes and their esters, such as ethyl fermentation, ethane fermentation, ethane monomethyl ether or ethyl ether, ketones, such as cyclohexyl, strong polar solvents For example, N-methyl-2-pyrrolidone, dimethyl sulfoxide or dimethylformamide, and unvaporized or cyclized vegetable oils, such as coconut gas or soybean oil; or water. Commonly used as a solid carrier for ash and dispersible powders are, for example, ground natural rocks such as calcite, talc, kaolin, montmorillonite or attapuUite. Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the notes on the back first (Fill in this page again) The other beneficial enhancement additives that can greatly reduce the response rate are natural (animal or plant) or synthetic phospholipids (from the list of brain phospholipids and lecithins), which can be obtained from, for example, soybeans. Depending on the nature of the active ingredient of formula I, a suitable interface activity «[compounds are non-male,» male and / or anionic interface active, which has excellent emulsification, dispersibility and grade properties. This understanding is Interfacial active thread also represents interfacial active_mixture. -38- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm). The A7 B7 is printed by the Consumer Labor Cooperative of the Central Bureau of Economic Development of the Ministry of Economic Affairs. ) Appropriate interfacial activity of yin and yin can be called water-soluble salts, but also can be called water-soluble synthetic interface-active compounds. Soap is Jin Yi salt, alkaline earth gold exhibition Salts or ammonium salts of substituted or unsubstituted high-number fatty acids (Ci 〇-C2 2), such as noodles or potassium * of oleic acid or stearic acid, or sodium salts or salts of natural fatty acid mixtures, which can be obtained from For example, coconut oil or tall oil. Mention may also be made of fatty acid methyl taurine. Suitable non-ionic surface active agents are mainly fatty strips or fatty acids, saturated or unsaturated fatty acids and alkyl groups. Phenol polydioxygenate derivatives, whose (fatty strips) free radicals may contain 3 to 30 bowel dioxygenate groups and 8 to 20 «sulfon atoms and alkyl phenol alkyl radicals contain 6 to 18 sickle atoms The examples of non-ionic interfacial activity include nonylphenol polyethylene glycol yeast, castor oil polyethylene glycol ether, polyoxygenated propylene / polyoxygenated ethylene adduct, tributylbenzene polyoxyethylene Acetate, polyoxirane and octylbenzene gas-based polyethylenyl acetate. Other suitable substances are fatty acids of polyoxyethylene sorbitan, such as polyoxyethylene sorbitan trioleate. __ The sub-interface activity is mainly quaternary ammonium, which contains at least one alkyl radical of 8 to 22 sulfon atoms as a substituent, which Possesses a low-yielding or free mandrel, benzyl or lower hydroxyalkyl radical as a further substituent. The》 is preferably in the form of a halide, methyl sulfate or ethyl sulfate, such as stearin Ammonium trimethylammonium cyanide or benzyl bis (2-aminoethyl) ammonium bromide. -39- This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) 丨: ----- -丨 installed ------ order ----- ^ line (please read the notes on the back before filling in this page) A7 _ B7 printed by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs For example, the agrochemical preparation includes 0.1 to 99%, especially 0.1 to 95% of the active ingredient of formula I. 99.9% to 1%, especially 99.9 to 5% solid or liquid added Use 0 to 25% and wait for 0.1 to 25% interface active rain. Although it is preferable to use a dense composition for a commercial product, a terminal de-energizer may routinely use a diluted composition. The composition may also include other additives, such as diazepam, defoaming agents, viscosity modifiers, binders, tackifiers, fertilizers or other active ingredients for special purposes. Formulations, i.e. compositions, split preparations or mixtures, which include the active ingredients of formula I and with or without solid alcohol or liquid additives, are prepared by conventional methods, such as mixing and / or grinding active ingredients and extensions », For example, solvents (mixtures), solid carriers, and, suitably, interface-active compounds (interactive agents). A preferred method in the field of protecting crops is on plant bushes (leaf applications), the frequency and rate of which depend on the degree of danger of contamination by special hazards. However, the active ingredient can also reach the plant via the root system (systemic action), which is like applying the liquid composition to moisten the plant location or adding the active ingredient in the form of solid brewing to the plant location, such as adding it to the soil, such as Granular form (soil application). For rice, such particles can be metered into a paddy field full of water. Alternatively, the compound of formula I can be applied to the seed stone fruit (coating) by dipping stone fruit in the liquid strontium composition or by coating with a solid composition. In principle, the use of the compound of formula I can protect any type -4 0- This &amp; Zhang scale applies the Chinese national standard (€ Can) 84 specifications (210 father 297 mm) IJ ------- ί I equipment ------ order ----- line (please read the precautions on the back before filling in this page) Α7 Β7 Fifth, the invention description (κ) plant propagation material. The compound of formula I is used as a pure active ingredient or preferably together with auxiliary additives commonly used in this art formula, and then processed in a known manner to obtain, for example, emulsifiable concentrates, directly sprayable or dilutable solutions, diluted emulsions , Wettable powder, soluble powder, dust and granules, there are also capsules containing polymer. Application methods include spraying, spraying, powdering, dispersing or pouring, and the composition are all formulated to meet the purpose and general requirements. A preferred application rate is 1 g to 2 kg of active ingredient / europium, 25 g to 800 g of active ingredient / mu, and 50 g to 40 g of active ingredient / mu. As a seed dressing product, the dosage per kilogram of seed is preferably from 0.001 g to 1.0 g of active ingredient. The following examples are intended to explain the present invention in more detail, and do not limit the present invention in any way. Preparation Example Ben Example Η _ 1: Preparation of IJ ------ 成-装 ------ 訂 ----- {'line (please read the precautions on the back before filling in this page) Printed by the Bureau of Standards and Staff Consumer Cooperative

-4 1- 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) Β7 五、 發明説明(4) 1. 32克羥基胺氫氯化物被加入5. 2克3 -甲氧 基一 2 — 〔(〔3_氣基一 2 -丁基)亞胺基〕氣基)鄰 甲苯基〕丙烯酸甲醸(EP-A- 3 7 0 6 2 9 , Ho. 156)在20毫升 吡啶中所形成溶液中。在3 0TC8I拌混合物6小時之後, 加入冰水,將數小時後所形成的结晶餅塊8濾,用水沖洗 结晶。以乙酵/水再結晶,得到4. 8克黄色结晶之3 — 甲氣基_2 - 〔(〔3 —羥基亞肢基一 2_ 丁基)亞胺基 〕氧基)鄰甲苯基〕丙烯_甲醱(^〇.1.73化合物),熔》 為 1 0 4 到 1 0 7 &quot;C。 實例Η _ 2 製備 ΗΧ '〇-4 1- This paper scale is applicable to the Chinese National Standard (CNS) Α4 specification (210X297mm) Β7. Description of the invention (4) 1. 32g of hydroxylamine hydrochloride is added to 5.2g of 3-methoxyl 2 — 〔([3_Amino-2-butyl) imino] amino) o-tolyl] methacrylic acid acrylate (EP-A-3 7 0 6 2 9, Ho. 156) in 20 ml of pyridine In the formed solution. After stirring the mixture at 30 ° C 8I for 6 hours, ice water was added, and the crystal cake 8 formed after several hours was filtered, and the crystal was washed with water. Recrystallized with ethyl yeast / water to obtain 4.8 g of yellow crystals of 3-methan-2--[([3-hydroxylidylene- 2_butyl) imino] oxy) o-tolyl] propene _Formaldehyde (^ 〇.1.73 compound), melted from 1 0 4 to 1 0 7 &quot; C. Example Η 2 Preparation Η Χ '〇

CF, (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 在一Κ力管中,将5毫升二甲基甲醣按加入〇. 2克 約65%氫化納懸浮物經己烷冲洗。然後,加入1. 6 克3 —甲氣基一 2 — 〔(〔3 —翔基亞胺基一 2 — 丁基) 亞胺基〕氣基)鄰甲苯基〕丙烯酸甲酯和1克2, 2 -42- 本紙張尺度適用中國國家標準(CNS ) Α4^8· ( 210X297公® ) 經濟部中央梂準局員工消費合作社印製 A7 B7_五、發明説明(巧) • 2~三氟乙基碘化物。等不再産生氳氣時,封閉屋力管 •在5〇它将該混合物攪拌5小時。然後•将反鼴溶液倒 入冰水中,用乙酸乙醣加以萃取,産物在矽®上以乙酸乙 酯/己烷(1 : 3&gt;作冲提液進行色層分析。製得1. 2 克的無色油之3—甲氣基一2— 〔(〔 (3—2, 2, 2 一三氟乙氧基亞胺基一 2 — 丁基)亞胺基〕氣基)鄰甲苯 基〕丙烯酸甲酯 (Ho. 1.74化合物)。 1H NMR(CDCls):兩但亞胺基取代甲基發生 化學位移:1. 99和2. 04ppm。 實例Η — 3 製備 (請先閱讀背面之注意事項再填寫本頁)CF, (please read the precautions on the back before filling out this page) Printed in a KK force tube by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, 5 ml of dimethyl methyl sugar is added to 0.2 g of about 65% hydrogenated The nano-suspension was washed with hexane. Then, add 1.6 g of 3-methylamino-2-([([3-pyridylimino-2-butyl) imino] amino) -o-tolyl] acrylic acid methyl ester and 1 g of 2, 2 -42- This paper scale is applicable to the Chinese National Standard (CNS) Α4 ^ 8 · (210X297 Gong ®) A7 B7_5 printed by the Consumers Cooperative of the Central Bureau of Economic Affairs of the Ministry of Economic Affairs. Invention Instructions (Qiao) • 2 ~ Trifluoroethyl Iodide. When the radon gas is no longer generated, close the housing tube • At 50, it will stir the mixture for 5 hours. Then • Pour the mole solution into ice water and extract with ethyl acetate. The product was analyzed on silica gel with ethyl acetate / hexane (1: 3>) as an eluent. Chromatography was performed to obtain 1.2 g Colorless oil of 3-methylamino-2-([([(3-2, 2, 2 trifluoroethoxyimino--2-butyl) imino] amino] o-tolyl) acrylic acid Methyl ester (Ho. 1.74 compound). 1H NMR (CDCls): Two but imino substituted methyl shift chemical shifts: 1.99 and 2. 04ppm. Example Η-3 Preparation (please read the notes on the back before filling in (This page)

15. 0克的對_甲基丙酚銅和20毫升II戊基亞硝 酸S於3 0毫升甲酵中所形成的溶掖被纽慢逐滴加入2 0 毫升甲基酸納(30%,於甲酵中)。攪拌混合物5小時 -43- 本紙張尺度適用中國國家標準(CNS ) A4规格(2丨〇X297公釐) ---I—.--^------^ I裝------訂-----J、 線 經濟部中央標準局員工消費合作社印製 A7 B7五、發明説明(^) 之後,逐滴加入30毫升水,接蓿用乙酸使混合物酸化。 用乙酸乙酯萃取混合物,用水冲洗萃取物,用硫酸納乾嫌 之,在真空中濃縮。殘留物被二乙基醚/正己烷再结晶, 得到無色结晶之α-羥基亞胺基_4-甲基丙酚謂,熔» 為1 22到1 24它。 8. 1克先前製得化合物和於40毫升毗啶中的4. 6 克鄰一甲基羥基胺氬«化物被回流1小時。在加入甲苯之 後,混合物在真空中囊缠,用水ft理.以乙酸乙醮萃取之 。用水冲洗有機相,在硫酸銪上乾燥,在臭空中濃缠。用 二乙基醚/正己烷再结晶,得到無色结晶之α—羥基亞胺 基一4 —甲基丙酣酮一氣一甲基肟,熔點為156到157C 0 1. 87克前述製得的肟和2. 58克2 — (ot —溴 一鄰一甲苯基)一 3 —甲氣基丙烯酸甲酯被加入0. 4 1 克氫化銷於25毫升N, N—二甲基甲蘭胺中所形成的懸 浮物,攪拌反應混合物3小時。然後用乙酸酸化之,用水 處理,用乙_乙_荦取。用鉋和硪酸氫納沖洗有櫬相兩次 ,用飽和氯化銷溶液沖洗一次。以無水硫酸«乾燥之後, 在真空中除去溶劑。從二乙基_/正己烷中结晶成無色结 晶的Η - 3化合物,其熔點為98到1 0 1 t:(No. 1.117 化合物)。 實例Η — 4 製備 -4 4 _ (請先閲讀背面之注意事項再填寫本頁) -裝. 4° 線. 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) 304C6C at _____B7五、發明説明(W )15. The dissolution of 0 g of copper p-methyl propofol and 20 ml of II amyl nitrite S in 30 ml of formazan was added slowly by dropwise addition of 20 ml of sodium methylate (30%, In the enzyme). Stir the mixture for 5 hours-43- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (2 丨 X297mm) --- I --.-- ^ ------ ^ I installed ----- -Subscribe ----- J. A7 B7 printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 5. After the description of the invention (^), add 30 ml of water drop by drop, and then acidify the mixture with acetic acid. The mixture was extracted with ethyl acetate, the extract was washed with water, dried with sodium sulfate, and concentrated in vacuo. The residue was recrystallized from diethyl ether / n-hexane to obtain colorless crystals of α-hydroxyimino-4-methylpropanol. The melting point was 1 22 to 1 24. 8. 1 g of the previously prepared compound and 4. 6 g of o-methylhydroxylamine in 40 ml of pyridine were refluxed for 1 hour. After the addition of toluene, the mixture was encapsulated in vacuum and extracted with ethyl acetate in water. Rinse the organic phase with water, dry it on europium sulfate, and entangle it in the smelly air. Recrystallized with diethyl ether / n-hexane to obtain colorless crystals of α-hydroxyimino-4-methylpropanone-gas monomethyloxime, melting point 156 to 157C 0 1.87 g And 2. 58 g of 2- (ot-bromo-o-tolyl) -3-methyl methyl acrylate was added to 0.4 1 g of hydrogenated pin in 25 ml of N, N-dimethylmethyl blue amine The resulting suspension was stirred for 3 hours. It is then acidified with acetic acid, treated with water, and taken with B_B_C. Rinse the shaved phase twice with a planer and sodium bicarbonate, and once with a saturated chlorinated pin solution. After drying with anhydrous sulfuric acid, the solvent was removed in vacuo. The H-3 compound crystallized from diethyl_ / n-hexane as a colorless crystal has a melting point of 98 to 101 t: (No. 1.117 compound). Example Η — 4 Preparation-4 4 _ (please read the precautions on the back before filling in this page)-installed. 4 ° line. The paper size is applicable to China National Standard (CNS) Α4 specification (210X297mm) 304C6C at _____B7 2. Description of Invention (W)

經濟部中央標準局員工消費合作社印製 0. 37克約65%氫化«懸浮物被己烷冲洗•加入 10毫升二甲基甲醯胺。將2. 59克之2— (2—澳甲 基苯基)二羥基乙酸一氣一甲基肟和2.42克2— ( 二苯基肼)一3-羥基亞胺丁烷的混合物加入此驗浮物中 ,接着使用熱空氣鼓風鑪將混合物加熱到40到50t!, 直到撖烈産生氫氣為止。然後在排除滬氣下»拌混合物1 小時,倒入冰水中。以乙酸乙明進行萃取,在矽驥上以乙 酸乙酯/己烷(1 : 2)作沖提液進行色靥分析,製得黄 色油之3. 7克2 — 〔 (〔 (3 —二苯基M—2 —丁基&gt; —亞胺基〕氣基)鄰一甲苯基〕二羥基乙酸甲酯 氣一甲 基肟(No. 2. 19化合物)。 1 Η N M R ( C D C 1 3 ):兩鶴亞胺基取代甲基發生 化學位移:1. 64和2. 12ppm。 實例Η — 5 製備 -45- (請先聞讀背面之注意事項再填寫本頁) •裝. 訂 線- 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) A7 B7 五、發明説明(μ )Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 0. 37 grams of approximately 65% hydrogenated «suspension was rinsed with hexane. Add 10 ml of dimethylformamide. Add a mixture of 2.59 grams of 2- (2-O-methylphenyl) diglycolic acid monomethyl oxime and 2.42 grams of 2- (diphenylhydrazine)-3-hydroxyiminebutane to this float In the next step, use a hot air blast furnace to heat the mixture to 40 to 50t! Until the hydrogen is generated. Then mix the mixture for 1 hour under the exclusion of Shanghai gas and pour into ice water. Extracted with ethyl acetate, on silica gel with ethyl acetate / hexane (1: 2) as an extraction solution for color analysis, to obtain 3.7 grams of yellow oil 2-((((3-diphenyl Group M-2-butyl-imino] amino] o-tolyl] dihydroxyacetic acid methyl ester gas monomethyl oxime (No. 2. 19 compound). 1 Η NMR (CDC 1 3): The chemical shifts of the two crane imino substituted methyl groups: 1. 64 and 2. 12 ppm. Example Η — 5 Preparation -45- (please read the precautions on the back side and then fill out this page) The scale is applicable to China National Standard (CNS) Α4 specification (210Χ297mm) A7 B7 5. Description of invention (μ)

1. 9克的2 — 〔 ( { (3 —二苯基肼一 2 —丁基) 一亞胺基}氣基)鄰_甲苯基〕二羥基乙酸甲酯 氣一甲 基肟在室溫下於10«升33%甲基胺溶液(於乙酵中) 中攪拌2小時。蒸發乙酵和遇量甲基胺,以二乙基酵吸收 殘留物,過濾溶液,蒸乾濾液,産物依然為結晶性固讎。 用己烷沖洗,製得淡灰色的1. 8克的2 — 〔(( 〔3 — 二苯基肼一 2 —丁基)_亞胺基}氣基)鄰一甲苯基〕二 羥基醯胺N甲基 氣一甲基肟(No. 3.19化合物),熔酤為 1 3 5 - 1 3 6 Ό 0 資例Η — 6 製備 I : ( I裝 訂 f 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製1. 9 grams of 2-[({(3-diphenylhydrazine-2-butyl) imino} amino] o-tolyl) methyl dihydroxyacetate gas monomethyloxime at room temperature Stir for 2 hours in 10 «L of 33% methylamine solution (in ethyl fermentation). Evaporation of ethyl yeast and encountering methylamine, absorption of the residue with diethyl yeast, filtration of the solution, and evaporation of the filtrate, the product is still crystalline solid. Rinse with hexane to prepare 1.8 g of 2-[((([3-diphenylhydrazine-2-butyl) -imino} amino] o-tolylyl] o-tolylyl] dihydroxyamide) N-methyl gas monomethyl oxime (No. 3.19 compound), the melting point is 1 3 5-1 3 6 Ό 0 Example Η — 6 Preparation I: (I binding f line (please read the notes on the back before filling in This page) Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

_ 4 6 _ 本紙張尺度逋用中國國家標準(CNS ) A4規格(210 X 297公釐) A7 ____B7 五、發明説明(叫) 将 1. 74 克式(AA)的 1 一 〔4 一 (2· 2 —二 氰琢丙基甲氣基)苯基〕丙烷一 1, 4二酮 1一 (氣一 甲基肟)一2—肟加入〇.13克氫化《(於25毫升N ,N —二甲基甲S胺中)·接著加入1. 5克式(BB) 的2— (2—溴甲基苯基)一3—甲®基丙烯酸甲酯·混 合物在室粗下被攪拌3小時。此混合物被乙酸酸化,加入 水和乙酸乙酯。分離水相,用飽和硪酸氫納溶掖冲洗有機 一次,於無水硫酸納上乾燥。在真空中蒸發溶劑,所得到 的殘留物在矽驥上以己烷/乙酸乙酯(3 : 1)進行純化 。所得到的標題化合物為油狀,在矽驥上(己烷/乙酸乙 酯溶液為3:1)進行色層分析以分離之,得到三種異構 物·異構物A,熔點86-88P·異檷物B:油,異構 物C (No.5.9化合物)。 (請先閱讀背面之注意事項再填寫本頁) 裝· 訂 經濟部中央標準局員工消費合作社印製_ 4 6 _ This paper scale adopts Chinese National Standard (CNS) A4 specification (210 X 297 mm) A7 ____B7 V. Description of the invention (called) 1. 74 grams (AA) of 1 one [4 one (2 · 2-Dyanocyanopropylmethanyl) phenyl] propane-1,4-dione 1- (gas-methyloxime) -2-oxime was added with 0.13 g of hydrogenated ((in 25 ml of N, N — Dimethyl methyl Samine) · Then add 1.5 g of formula (BB) of 2- (2-bromomethylphenyl)-3-methyl methyl acrylate · The mixture was stirred for 3 hours in the crude room . This mixture was acidified with acetic acid, and water and ethyl acetate were added. Separate the aqueous phase, rinse the organic matter once with saturated sodium bicarbonate, and dry over anhydrous sodium sulfate. The solvent was evaporated in vacuo, and the resulting residue was purified on silica gel with hexane / ethyl acetate (3: 1). The title compound was obtained as an oil, which was separated by chromatography on silica gel (hexane / ethyl acetate solution 3: 1) to obtain three isomers · isomer A, melting point 86-88P · iso Bilder B: oil, isomer C (No. 5.9 compound). (Please read the precautions on the back before filling out this page) Binding · Order Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7 B7 五、發明説明(# ) 以下的化合物可依類似上述方法加以製備:(编寫: Me為甲基,Et為乙基.△為琛丙基,Ph為苯基, m p為箱黏) N M R :化學位移以S( PPm)(於CDCI3)表 7J\ 〇 1 n^i nn ^^^^1 Β^ϋΒ fem- mV nn HI n^i - 、 ml • . ^ i ^ (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 48 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) J04860 五、發明説明(w 表1 A7 B7This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) A7 B7 5. Invention description (#) The following compounds can be prepared in a similar manner to the above method: (Compiled: Me is methyl, Et is ethyl. △ is propyl group, Ph is phenyl group, mp is box viscosity) NMR: chemical shift is S (PPm) (in CDCI3) Table 7J \ 〇1 n ^ i nn ^^^^ 1 Β ^ ϋΒ fem- mV nn HI n ^ i-, ml •. ^ I ^ (Please read the precautions on the back before filling in this page) Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 48 This paper standard is applicable to the Chinese National Standard (CNS) Α4 specification (210X297 Mm) J04860 V. Description of invention (w Table 1 A7 B7

H,CH, C

A r3 經濟部中央標準局員工消費合作杜印製 實例 A R i Rz 83 或nr3 R4 編號 1.1 NMe Me He 6-CF3 -2-at啶基 1.2 NHe H Me 6-CF3 -2-llt啶基 1 . 3 NMe Me △ 6-CF3 -2-吡啶基 1.4 NMe Me H 苯基 1.5 NHe Me Me 苯基 1.6 NMe Δ Me 苯基 1.7 NNe Me Me 4-CF3 -2-¾啶基 1.8 NMe H Me 4-CF3 -2-¾啶基 1.9 NMe △ △ 苯基 1.10 NMe Me Me 5- CF3 -2 - Itt疲基 物理資料 -49 » * .17/2.1 2.09/2.1 .p 100t 2.17/2.18 I ^ (' I裝 訂 線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X29*7公釐) 五、發明説明Uf) A7 B7 經濟部中央標準局員工消費合作社印製 1.11 NNe H Me 5-CF3 -2-¾ 啶基 1.12 -- H Me 4-(1, 2,4-三睡基) 1.13 -- NMe Me 4- (1 , 2 , 4-三唑基) 161-163^ 1.14 -- Me △ 4-(1, 2,4-三唑基) 1.15 -- Me △ 4-嗎啉基 1.16 -- Me Me 4-嗎啉基 113t: 1.17 -- H Me 4-瞟啉基 1.18 NPh« H Me 苯基 1.19 NPh» Me Me 苯基 1.74/2.22 1.20 NPh# Me △ 苯基 1.21 HPh# △ Me 苯基 1.22 NMe Me Me 2-硝基苯基 1.93/2.06 1.23 MMe H Me 2-硝基苯基 1.24 0 Me Me Me 76-78¾ 1.25 0 H Me Me 1.97/7.68 1.26 0 △ Me Me 1.96/2.00 1.27 0 Me △ Me 6 0 - 6 2 ¾ 1.28 0 Me H Me 1.29 NHe H Me 3-CF3 -2-lft 啶基 1.30 NMe Me Me 3-CF3 -2-吡啶基 2.06/2.18 1.31 NHe △ Me 3-CF3 -2-吡啶基 1.32 NMe △ Me 3-硝基-2-¾啶基 1.33 NMe H Me 3-硝基-2-吡啶基 -50- — ^------{ —裝------訂-----線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(W) A7 B7 經濟部中央標準局員工消費合作社印製 1.34 NMe Me Me 3-硝基 -2-吡啶基 1.94/2.26 1.35 NMe Me Me 2-CF3 -苯基 1.85/2.10 1.36 NMe Me △ 2-CF3 -苯基 1.37 NNe H He 2-CF3 -苯基 1.38 NMe Me Me 3-CF3 -苯基 1.39 NNe Me △ 3-CF3 -苯基 1.40 NHe H Me 4-CF3 -苯基 1.41 NMe Me Me 4- CF3 -苯基 1.42 NMe Me Me 2-氛苯基 1.73/2.13 1.43 NHe Me Me 3-氯苯 基 2.12/2.17 1.44 NMe H He 4-氛苯 基 1.45 NNe He He 4-氰苯基 2.10/2.15 1.46 0 Me Me 苯基 2.14/2.22 1.47 0 Me Δ 苯基 1.48 0 Me Me 苄基 1 0 6 - 1 0 8 10 1.49 0 Me Me Ht 1.92/1.95 1.50 0 H Me Et 1.51 0 △ Me Et 1.52 0 Me Δ Et 1.53 0 He H Et 1.54 0 H Me 甲氧基甲基 1.55 0 Me He 甲氣基甲基 83-84 ^ 1.56 0 He Δ 甲氧基甲基 一 51- ; ( —裝 τ口 ^線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 五、發明説明(ui ) A7 B7 經濟部中央標準局員工消費合作社印製 1.57 0 △ Me 甲氣基甲基 1.58 0 Me He 乙氣基甲基 2.04/2.04 1.59 0 Me Me 氱基甲基 1.60 0 Me Me 氡基甲基 2.04/2.04 1.61 - Δ Me 氰基甲基 1.62 - Me Me 氮雜箪基 1.63 - Me Me 锨啶烷基 1 . 64 0 Me Me 吡啶烷基 1.65 0 H Me 三级丁基 1.66 0 Me Me 三级丁基 1.96/2.04 1.67 0 Me Me 炔丙基 114-115¾ 1.68 0 Δ Me 炔丙基 1.69 0 Me Δ 炔丙基 1.70 0 Me Me 2 , 2-二氯琛 丙基甲基 2.02/2.02 1.71 0 △ Me 2 , 2-二氛環 丙基甲基 1.72 0 Me Me Η 1.73 0 Me He Η 104-1071 1.74 0 Me Me CF3 CHz 1.99/2.04 1.75 0 Δ Me CF3 ch2 1.76 0 Me H CF3 CHz 1.77 0 Me H CF3 CHz CH2 -52- ^^^1 ^^^1 i nn m m^i ^^^1 ^^1 t^i ^1^1 r^n Hi I i ^^^1 1^^1 1^^1 I In - J. I m· 1^^1 ^^^1 ^1. - • . J 务 i-4鱗 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(叫) A7 B7 經濟部中央標準局員工消費合作社印製 1.78 0 Me Me cf3 ch2 ch2 1.79 0 Me Me CF3 CH2 CHz CHz 2.10/2.13 1.80 0 Δ Me cf3 ch2 ch2 ch2 1.81 0 NHe Me Me 94- 98¾ 1.82 0 NMe Δ Me 1.83 0 Me Me ch2 -cci=ch2 80¾ 1.84 0 △ He CHz -CC1=CHZ 1.85 0 Me Me 丙基 1.86 0 He Ne 丁基 36- 38t: 1.87 0 Me Me 己基 1.99/2.01 1.88 0 He Me 甲氧基羰基甲基 90- 93 ¾ 1.89 0 H Me 甲氣基羰基甲基 1.90 0 Me Me 3-氟苄基 2.00/2.04 1.91 0 Me Ne 4-氱苄基 1.92 0 He Me 2-氛苄基 1.93 0 Me Me 2-CFs -苄基 1.94 0 Me Me 3-CFs -苄基 56-58TC 1.95 0 Me Me 4-CF3 -苄基 1.96 0 Me Me 3,4-二氨苄基 1.97 0 Me Ne 2 , 4 , 6-三甲基苄基 1.98 0 Me Me 4-氨-2-硝基苄基 1.99 0 Me Me 3-甲氧基苄基 1.100 0 Me Me 2-苯基丙基 1.97/2.02 -53- (請先閲讀背面之注意事項再填寫本頁) -----^--‘------^ I 裝------訂---- .線 _ 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(4) A7 B7 經濟部中央標準局員工消費合作社印製 1.10 1 0 Me Me 3-苯基丙基 1.102 0 Me Me 2-(4-硝基苯 基)乙基 1.103 0 Me He 2-(2-CF3 -苯基) 乙基 1.104 0 Me Me 2-(4-甲氣基苯 基)乙基 1.105 0 Me Me 2-氛-6-瓤苄基 1.106 0 Me He 3 , 4-次甲基二 氣基苄基 1.107 0 He Me 2-氣基苄基 1.108 0 He Me 2-(4-氣苯基)乙基 1.109 0 Me Me 氰基丙基甲基 2.01/2.01 1.110 0 Me Me 2- (1 , 3-二噁茂 基)甲基 1.111 0 Me Me 2,2,3,3,-四氟琢 丁基甲基 1.112 0 Me Me « -氟乙氣基羰 基甲基 1.113 0 Me 2-雄盼基 Me 2.06/2.10 2 . 20(E/Z) 1.114 0 Me 4-甲基 Et 2.12 苯基 -54- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 1^1 H —^ϋ nn ί t^—Λ ί ^^^1 ^^^1 ^^^1 ^ϋ ^ϋ I , il^i (n n . »s^« .—^¾. 、1-4^ (請先閲讀背面之注意事項再填寫本頁) 五、發明説明(β ) A7 B7 1.115 NMe Me 4-甲基 He 2. 1〇(異構 苯基 2.08(異構 1.116 0 Me Me CHZ FCH2 50-5 It: 1.117 0 Me He 2-(4-¾啉基)乙基 1.99/2.01 1.118 0 Me Me 吡咯基 89-9 It: 1.119 0 Me He 2-(1-报格院基) 乙基 1.120 0 Me Me 2-氟苄基 9 3- 9 6 ¾ 1.121 0 Me Me 4-氟苄基 104-106¾ «» R 1 /Rz 或R3的·. P .或1 H NMR b_IS. (請先閱讀背面之注意事項再填寫本頁) 裝. 、-° 線 經濟部中央標準局—工消費合作社印裝 -55-本紙張尺度適用中國國家揉準(CNS ) A4規格(210 X 297公釐) 304860 A7 B7 五、發明説明(&gt;) 表2 N COOCH3A r3 Examples of du printing of consumer cooperation in the Central Bureau of Standards of the Ministry of Economy AR i Rz 83 or nr3 R4 No. 1.1 NMe Me He 6-CF3 -2-at pyridyl 1.2 NHe H Me 6-CF3 -2-llt pyridyl 1. 3 NMe Me △ 6-CF3 -2-pyridyl 1.4 NMe Me H phenyl 1.5 NHe Me Me phenyl 1.6 NMe Δ Me phenyl 1.7 NNe Me Me 4-CF3 -2-¾ pyridyl 1.8 NMe H Me 4-CF3 -2-¾ Pyridinyl 1.9 NMe △ △ Phenyl 1.10 NMe Me Me 5- CF3 -2-Itt Fatigue Physical Data -49 »* .17 / 2.1 2.09 / 2.1 .p 100t 2.17 / 2.18 I ^ ('I binding Line (please read the precautions on the back before filling in this page) This paper scale is applicable to the Chinese National Standard (CNS) Α4 specification (210X29 * 7mm) V. Description of invention Uf) A7 B7 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards 1.11 NNe H Me 5-CF3 -2-¾ pyridyl 1.12-H Me 4- (1, 2,4-trisyl) 1.13-NMe Me 4- (1, 2, 4-triazolyl) 161-163 ^ 1.14-Me △ 4- (1, 2,4-triazolyl) 1.15-Me △ 4-morpholinyl 1.16-Me Me 4-morpholinyl 113t: 1.17-H Me 4 -Oxolinyl 1.18 NPh «H Me Phenyl 1.19 NPh» Me Me Phenyl 1.74 /2.22 1.20 NPh # Me △ Phenyl 1.21 HPh # △ Me Phenyl 1.22 NMe Me Me 2-Nitrophenyl 1.93 / 2.06 1.23 MMe H Me 2-Nitrophenyl 1.24 0 Me Me Me 76-78¾ 1.25 0 H Me Me 1.97 / 7.68 1.26 0 △ Me Me 1.96 / 2.00 1.27 0 Me △ Me 6 0-6 2 ¾ 1.28 0 Me H Me 1.29 NHe H Me 3-CF3 -2-lft pyridyl 1.30 NMe Me Me 3-CF3- 2-pyridyl 2.06 / 2.18 1.31 NHe △ Me 3-CF3 -2-pyridyl 1.32 NMe △ Me 3-nitro-2-¾-pyridyl 1.33 NMe H Me 3-nitro-2-pyridyl-50-- ^ ------ {—install ------ order ----- line (please read the precautions on the back before filling in this page) This paper size is applicable to China National Standard (CNS) A4 specification (210X297 Mm) V. Description of invention (W) A7 B7 Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 1.34 NMe Me Me 3-nitro-2-pyridyl 1.94 / 2.26 1.35 NMe Me Me 2-CF3 -phenyl 1.85 / 2.10 1.36 NMe Me △ 2-CF3 -phenyl 1.37 NNe H He 2-CF3 -phenyl 1.38 NMe Me Me 3-CF3 -phenyl 1.39 NNe Me △ 3-CF3 -phenyl 1.40 NHe H Me 4-CF3 -benzene Base 1.41 NMe Me Me 4- CF3 -phenyl 1.42 NMe Me Me 2-chlorobenzene Base 1.73 / 2.13 1.43 NHe Me Me 3-chlorophenyl 2.12.2.17 1.44 NMe H He 4-aminophenyl 1.45 NNe He He 4-cyanophenyl 2.10 / 2.15 1.46 0 Me Me Phenyl 2.14 / 2.22 1.47 0 Me Δ Phenyl 1.48 0 Me Me Benzyl 1 0 6-1 0 8 10 1.49 0 Me Me Ht 1.92 / 1.95 1.50 0 H Me Et 1.51 0 △ Me Et 1.52 0 Me Δ Et 1.53 0 He H Et 1.54 0 H Me Methoxy Methylmethyl 1.55 0 Me He Methylmethyl 83-84 ^ 1.56 0 He Δ Methoxymethyl 51-; (—Install τ mouth ^ line (please read the precautions on the back before filling this page) This The paper scale is applicable to the Chinese National Standard (CNS) Α4 specification (210Χ297mm) 5. Description of the invention (ui) A7 B7 Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 1.57 0 △ Me Methylmethyl 1.58 0 Me He Methylmethyl 2.04 / 2.04 1.59 0 Me Me Methylmethyl 1.60 0 Me Me Radonyl 2.04 / 2.04 1.61-Δ Me Cyanomethyl 1.62-Me Me Azatriyl 1.63-Me Me Succinylalkyl 1 . 64 0 Me Me pyridinyl 1.65 0 H Me tertiary butyl 1.66 0 Me Me tertiary butyl 1.96 / 2.04 1.67 0 Me Me propargyl 114-115¾ 1.68 0 Δ Me propargyl 1.69 0 Me Δ propargyl 1.70 0 Me Me 2, 2-dichloropropenylmethyl 2.02 / 2.02 1.71 0 △ Me 2, 2-dichlorocyclopropylmethyl 1.72 0 Me Me Η 1.73 0 Me He Η 104-1071 1.74 0 Me Me CF3 CHz 1.99 / 2.04 1.75 0 Δ Me CF3 ch2 1.76 0 Me H CF3 CHz 1.77 0 Me H CF3 CHz CH2 -52- ^^^ 1 ^^ ^ 1 i nn mm ^ i ^^^ 1 ^^ 1 t ^ i ^ 1 ^ 1 r ^ n Hi I i ^^^ 1 1 ^^ 1 1 ^^ 1 I In-J. I m · 1 ^^ 1 ^^^ 1 ^ 1.-•. J Wu i-4 scale (please read the precautions on the back before filling in this page) This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) V. Invention Description (called) A7 B7 Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy 1.78 0 Me Me cf3 ch2 ch2 1.79 0 Me Me CF3 CH2 CHz CHz 2.10 / 2.13 1.80 0 Δ Me cf3 ch2 ch2 ch2 1.81 0 NHe Me Me 94- 98¾ 1.82 0 NMe Δ Me 1.83 0 Me Me ch2 -cci = ch2 80¾ 1.84 0 △ He CHz -CC1 = CHZ 1.85 0 Me Me propyl 1.86 0 He Ne butyl 36- 38t: 1.87 0 Me Me hexyl 1.99 / 2.01 1.88 0 He Me Methoxycarbonylmethyl 90- 93 ¾ 1.89 0 H Me Methoxy Methylmethyl 1.90 0 Me Me 3-fluorobenzyl 2.00 / 2.04 1.91 0 Me Ne 4- 氱 benzyl 1.92 0 He Me 2-aminobenzyl 1.93 0 Me Me 2-CFs -benzyl 1.94 0 Me Me 3-CFs -Benzyl 56-58TC 1.95 0 Me Me 4-CF3 -benzyl 1.96 0 Me Me 3,4-diaminobenzyl 1.97 0 Me Ne 2, 4, 6-trimethylbenzyl 1.98 0 Me Me 4-amino- 2-nitrobenzyl 1.99 0 Me Me 3-methoxybenzyl 1.100 0 Me Me 2-phenylpropyl 1.97 / 2.02 -53- (please read the precautions on the back before filling this page) ---- -^ --'------ ^ I installed ------ ordered ---- .Line_ This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) V. Description of invention ( 4) A7 B7 Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy 1.10 1 0 Me Me 3-phenylpropyl 1.102 0 Me Me 2- (4-nitrophenyl) ethyl 1.103 0 Me He 2- (2- CF3 -phenyl) ethyl 1.104 0 Me Me 2- (4-methylphenyl) ethyl 1.105 0 Me Me 2-hydrogen-6-flour benzyl 1.106 0 Me He 3, 4-methine digas Benzyl 1.107 0 He Me 2-aminobenzyl 1.108 0 He Me 2- (4-aminophenyl) ethyl 1.109 0 Me Me cyanopropylmethyl 2.01 / 2.01 1.110 0 Me Me 2- (1,3-dioxenyl) methyl 1.111 0 Me Me 2,2,3,3, -tetrafluoroisobutylmethyl 1.112 0 Me Me «-fluoroethylcarbonylcarbonylmethyl 1.113 0 Me 2-andronyl Me 2.06 / 2.10 2 .20 (E / Z) 1.114 0 Me 4-methyl Et 2.12 Phenyl-54- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 1 ^ 1 H — ^ ϋ nn ί t ^ —Λ ί ^^^ 1 ^^^ 1 ^^^ 1 ^ ϋ ^ ϋ I, il ^ i (nn. »S ^« .— ^ ¾., 1-4 ^ (Please read the precautions on the back before filling this page) V. Description of the invention (β) A7 B7 1.115 NMe Me 4-methyl He 2. 1〇 (isomeric phenyl 2.08 (isomeric 1.116 0 Me Me CHZ FCH2 50-5 It: 1.117 0 Me He 2- (4-¾olinyl) ethyl 1.99 / 2.01 1.118 0 Me Me Pyrrolyl 89-9 It: 1.119 0 Me He 2- (1-Reporter) ethyl 1.120 0 Me Me 2-fluorobenzyl 9 3- 9 6 ¾ 1.121 0 Me Me 4-fluorobenzyl 104-106¾ «» R 1 / Rz or R3. P. Or 1 H NMR b_IS. (Please read first (Notes on the back and then fill out this page) Pack.,-° Line Printed by the Central Standards Bureau of the Ministry of Economy-Industrial and Consumer Cooperatives -55- This paper size is suitable for Chinese countries Quasi (CNS) A4 size (210 X 297 mm) 304860 A7 B7 V. invention is described (&gt;) Table 2 N COOCH3

(請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 實 例 A R i Rz R3 物理 資料 或NR3 r4 编 號 2 1 NMe Me Me 6-CF3 -2 -at 啶 基 2 . 2 NMe H Me 6-CF3 -2 -at 啶 基 2 . 3 NMe Me △ 6-CF3 -2 -at 啶 基 2 . 4 NMe Me H 苯基 2 . 5 NMe Me Me 苯基 87 -88¾ 2 . 6 NMe Δ Me 苯基 2 . 7 NMe Me Me 4-CF3 -2-¾ 啶 基 2 . 8 NMe H Me 4-CF3 -2 -¾ 啶 基 2 . 9 NMe △ Δ 苯基 2 . 10 NMe Me Me 5-CF3 -2 -吡 啶 基 -56- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(Jr丨) A7 B7 經濟部中央標準局員工消費合作社印製 2.11 NMe H Me 5 - C F 3 - 2 -吡啶基 2.12 — H Me 4-(1, 2,4-三唑基) 2.13 -- NMe He 4- (1 , 2 ,4-三畦基) 2.14 -- He Δ 4-(1, 2,4-三唑基) 2.15 -- Me △ 4-嗎啉基 2.16 -- Me Me 4-瞟啉基 2.17 -- H He 4-嗎啉基 2.18 NPh# H Me 苯基 2.19 HPh» Me Me 苯基 1.64/2.12 2.20 NPh» Me △ 苯基 2.21 NPh* Δ He 苯基 2.22 NMe Me Me 2-硝基苯基 2.23 NMe H Me 2-硝基苯基 2.24 0 Me Me Me 104-106¾ 2.25 0 H Me Me 2.26 0 △ He Me 1.92/1.97 2.27 0 Me △ Me 6 7- 7 0 ¾ 2.28 0 Me H Me 2.29 NMe H He 3-CF3 -2-ftt 啶基 2.30 NMe Me Me 3-CF3 -2-毗啶基 2.31 NHe △ Me 3-CF3 -2-ltt 啶基 2.32 NMe Δ Me 3-硝基-2-吡啶基 2.33 NMe H Me 3-碼基- 2- lfii淀基 -57- —.I------·(· I 裝------訂-----^ 線 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7 B7 五、發明説明(j^) 經濟部中央標準局員工消費合作杜印製 2.34 NNe Me Me 3-硝基-2-ftt啶基 2.35 NMe Me Me 2-CF3 -苯基 2.36 NMe Me △ 2_CF3 -苯基 2.37 ΝΗβ H Me 2-CF3 -苯基 2.38 NMe He Me 3-CF3 -苯基 2.39 NMe Me Δ 3-CF3 -苯基 2.40 NNe H Me 4 - C F 3 -苯基 2.41 NMe Me He 4-CF3 -苯基 2.42 NMe Me Me 2-氯苯基 81Ό 2.43 NMe Me Me 3 -氯苯基 2.10/2.13 2.44 NNe H Me 4-氯苯基 2.45 NMe Me Me 4-氛苯基 2.08/2. 13 2.46 0 He Me 苯基 89-9 0Ό 2.47 0 Me Δ 苯基 2.48 0 Me Me 苄基 2.49 0 Me Me Et 2.50 0 H Me Et 2.51 0 Δ Me Et 2.52 0 He Δ Et 2.53 0 Me H Et 2.54 0 H Me 甲氣基甲基 2.55 0 Me Me 甲氧基甲基 87-88t: 2.56 0 Me △ 甲氣基甲基 -58- (請先閱讀背面之注意事項再填寫本頁) ——裝--- 訂-----{.線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公嫠) 304860 A7 B7五、發明説明) 經濟部中央標準局員工消費合作社印製 2.57 0 △ Me 甲駕基甲基 2.58 0 Me Me 乙氣基甲基 2.59 0 Me Me 氰基甲基 2.60 0 Me Me m基甲基 9 4 - 95 ¾ 2.61 - Δ Me 氱基甲基 2.62 - Me Me 氮雜薙基 2.63 - He Me 哌啶烷基 2.64 0 Me He 吡啶烷基 2.65 0 H Me 三级丁基 2.66 0 Me He 三级丁基 1.93/2.02 2.67 0 Me Me 炔丙基 120-122¾ 2.68 0 △ Me 炔丙基 2.69 0 Me Δ 炔丙基 2.70 0 Me Me 2 , 2-二氨琛 丙基甲基 1.99/1.99 2.71 0 Δ Me 2 , 2-二氛琢 丙基甲基 2.72 0 He Me Η 2.73 0 Me Me Η 114-116¾ 2.74 0 Me Me CF3 CHz 52-53¾ 2.75 0 Δ Me CF3 CHz 2.76 0 He H cf3 ch2 2.77 0 Me H CF3 CH2 CHz -59- (請先閱讀背面之注意事項再填寫本頁) - 1 ^^^1 - - -- I 1^1 —^n ^^^1 n^i ^^^1 ^^^1 111 1 、一 - - 1: ^1^1 In _ 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7 B7 五、發明説明(# ) 經濟部中央標準局員工消費合作社印製 2 . 78 0 Me Me CF3 CHz CHz 2.79 0 Me Me cf3 ch2 ch2 ch2 86¾ 2.80 0 Δ Me CF3 CHz CHz CHz 2.81 0 NHe Me Me 80-enc 2.82 0 NMe △ He 2.83 0 Me He CHZ -CC1 = ch2 66Ό 2.84 0 △ Me CH2 -CC1 = CHZ 2.85 0 Me Me 丙基 2.86 0 Me Me 丁基 58- 6 2 TC 2.87 0 Me Me 己基 50- 5 3 ¾ 2.88 0 Me Me 甲氣基羰基甲基 1.96/2.04 2.89 0 H Me 甲氧基羰基甲基 2.90 0 Me Me 3-氟苄基 2.91 0 Me Me 4-氮苄基 2.92 0 Me Me 2-氛苄基 2.93 0 Me He 2-CF3 -苄基 2.94 0 He Me 3-CF3 -苄基 87-88¾ 2.95 0 Me Me 4-CF3 -苄基 2.96 0 Me Me 3,4-二氱苄基 2.97 0 Me Me 2,4,6-三 甲基苄基 2.98 0 Me Me 4-氰-2-硝基苄基 2.99 0 He Me 3-甲氣基苄基 2.100 0 Me Me 2-苯基丙 基 -60- (請先閱讀背面之注意事項再填寫本頁) 裝------訂-----.線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(β) A7 B7 經濟部中央標準局員工消費合作社印製(Please read the precautions on the back before filling in this page) Printed example of AR i Rz R3 physical data or NR3 r4 number 2 1 NMe Me Me 6-CF3 -2 -at -pyridyl 2 . 2 NMe H Me 6-CF3 -2 -at pyridyl 2. 3 NMe Me △ 6-CF3 -2 -at pyridyl 2. 4 NMe Me H phenyl 2.5 NMe Me Me phenyl 87 -88¾ 2. 6 NMe Δ Me phenyl 2. 7 NMe Me Me 4-CF3 -2-¾ pyridyl 2. 8 NMe H Me 4-CF3 -2-¾ pyridyl 2. 9 NMe △ Δ phenyl 2. 10 NMe Me Me 5-CF3 -2 -Pyridyl-56- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) V. Description of the invention (Jr 丨) A7 B7 Printed by the employee consumer cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 2.11 NMe H Me 5-CF 3-2 -pyridyl 2.12 — H Me 4- (1, 2,4-triazolyl) 2.13-NMe He 4- (1, 2, 4-triazolyl) 2.14-He Δ 4- (1, 2,4-triazolyl) 2.15-Me △ 4-morpholinyl 2.16-Me Me 4-oxolinyl 2.17-H He 4-morpholinyl 2.18 NPh # H Me benzene Base 2.19 HPh »Me Me phenyl 1.64 / 2.12 2.20 NPh »Me △ phenyl 2.21 NPh * Δ He phenyl 2.22 NMe Me Me 2-nitrophenyl 2.23 NMe H Me 2-nitrophenyl 2.24 0 Me Me Me 104-106¾ 2.25 0 H Me Me 2.26 0 △ He Me 1.92 / 1.97 2.27 0 Me △ Me 6 7- 7 0 ¾ 2.28 0 Me H Me 2.29 NMe H He 3-CF3 -2-ftt pyridyl 2.30 NMe Me Me 3-CF3 -2- Pyridinyl 2.31 NHe △ Me 3-CF3 -2-ltt pyridyl 2.32 NMe Δ Me 3-nitro-2-pyridyl 2.33 NMe H Me 3-codeyl- 2- lfii yl-57- —.I- ----- · (· I installed ------ ordered ----- ^ line (please read the precautions on the back before filling in this page) This paper size is applicable to China National Standard (CNS) A4 specification ( 210X297mm) A7 B7 V. Description of invention (j ^) DuPont Printing by Staff Consumption Cooperation of the Central Standards Bureau of the Ministry of Economic Affairs 2.34 NNe Me Me 3-nitro-2-ftt pyridyl 2.35 NMe Me Me 2-CF3 -phenyl 2.36 NMe Me △ 2_CF3 -phenyl 2.37 ΝΗβ H Me 2-CF3 -phenyl 2.38 NMe He Me 3-CF3 -phenyl 2.39 NMe Me Δ 3-CF3 -phenyl 2.40 NNe H Me 4-CF 3 -phenyl 2.41 NMe Me He 4-CF3 -phenyl 2.42 NMe Me Me 2-chlorophenyl 81Ό 2.43 NMe Me Me 3 -chlorophenyl 2.10 / 2.13 2.44 NNe H Me 4-chlorophenyl 2.45 NMe Me Me 4-aminophenyl 2.08 / 2. 13 2.46 0 He Me phenyl 89-9 0Ό 2.47 0 Me Δ phenyl 2.48 0 Me Me benzyl 2.49 0 Me Me Et 2.50 0 H Me Et 2.51 0 Δ Me Et 2.52 0 He Δ Et 2.53 0 Me H Et 2.54 0 H Me Methylmethyl 2.55 0 Me Me Methoxymethyl 87 -88t: 2.56 0 Me △ Methoxymethyl-58- (please read the precautions on the back before filling in this page) ——Installation --- Order ----- {. The size of the paper in line is applicable to Chinese national standards (CNS) A4 specification (210X297 gongnai) 304860 A7 B7 V. Invention description) Printed by the Consumer Standardization Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 2.57 0 △ Me Methylmethyl 2.58 0 Me Me Ethylmethyl 2.59 0 Me Me Cyanomethyl 2.60 0 Me Me Methyl methyl 9 4-95 ¾ 2.61-Δ Me Trimethyl 2.62-Me Me Azalyl 2.63-He Me Piperidinyl 2.64 0 Me He Pyridinyl 2.65 0 H Me tertiary butyl 2.66 0 Me He tertiary butyl 1.93 / 2.02 2.67 0 Me Me propargyl 120-122¾ 2.68 0 △ Me propargyl 2.69 0 Me Δ propargyl 2.7 0 0 Me Me 2, 2-diaminopropylmethyl 1.99 / 1.99 2.71 0 Δ Me 2, 2-diaminopropylmethyl 2.72 0 He Me Η 2.73 0 Me Me Η 114-116¾ 2.74 0 Me Me CF3 CHz 52-53¾ 2.75 0 Δ Me CF3 CHz 2.76 0 He H cf3 ch2 2.77 0 Me H CF3 CH2 CHz -59- (Please read the precautions on the back before filling this page)-1 ^^^ 1--- I 1 ^ 1 — ^ n ^^^ 1 n ^ i ^^^ 1 ^^^ 1 111 1 、 一--1: ^ 1 ^ 1 In _ The size of the linear paper is in accordance with the Chinese National Standard (CNS) A4 specification ( 210X297 mm) A7 B7 V. Description of invention (#) Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy 2.78 0 Me Me CF3 CHz CHz 2.79 0 Me Me cf3 ch2 ch2 ch2 86¾ 2.80 0 Δ Me CF3 CHz CHz CHz 2.81 0 NHe Me Me 80-enc 2.82 0 NMe △ He 2.83 0 Me He CHZ -CC1 = ch2 66Ό 2.84 0 △ Me CH2 -CC1 = CHZ 2.85 0 Me Me propyl 2.86 0 Me Me butyl 58- 6 2 TC 2.87 0 Me Me Hexyl 50- 5 3 ¾ 2.88 0 Me Me Methoxycarbonylmethyl 1.96 / 2.04 2.89 0 H Me Methoxycarbonylmethyl 2.90 0 Me Me 3-fluorobenzyl 2.91 0 Me Me 4-nitrobenzyl 2.92 0 Me Me 2-aminobenzyl 2. 93 0 Me He 2-CF3 -benzyl 2.94 0 He Me 3-CF3 -benzyl 87-88¾ 2.95 0 Me Me 4-CF3 -benzyl 2.96 0 Me Me 3,4-dihydroxybenzyl 2.97 0 Me Me 2 , 4,6-trimethylbenzyl 2.98 0 Me Me 4-cyano-2-nitrobenzyl 2.99 0 He Me 3-methoxybenzyl 2.100 0 Me Me 2-phenylpropyl-60- (please Read the precautions on the back first and then fill out this page) Binding ------ Order -----. The size of the line paper is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) V. Description of the invention (β) A7 B7 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

2.101 0 Me Me 3-苯基丙基 2.102 0 Me Me 2-(4-硝基苯 基)乙基 2.103 0 Me Me 2- (2-CF3 -苯基) 乙基 2.104 0 Me Me 2-(4-甲氣基苯 基)乙基 2.105 0 Me Me 2-氯-6-氟苄基 2.106 0 He He 3,4 -次甲基二 氣基苄基 2.107 0 Me Me 2-氰基苄基 2.108 0 Me Me 2-(4-氮苯基)乙基 2.109 η Me Me 氰基丙基甲基 1.98/1.98 2.110 0 Me Me 2-(1,3-二噁茂 基)甲基 2.111 0 Me Me 2 , 2 , 3 , 3 ,-四氟琛 丁基甲基 2.112 0 Me Me Msstsf —J* -ΛΛ- yuj ot 乙氧*玻 基甲基 2.113 0 He 2-噻盼基 Me 83-86 Ό 2.114 0 Me 4-甲基 Et 9 4 - 9 6 TC 苯基 -61- 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) (請先閲讀背面之注意事項再填寫本頁) -----^ I 裝------訂-----^ --^ A7 B7 五、發明説明(0 ) 經濟部中央標準局員工消費合作社印製 2.115 NNe Me 4 -甲基 Me 苯基 2.116 0 Me Me CH2 FCHZ 6 2 - 6 3 TC 2.117 0 Me Me 2-(4-嗎啉基)乙基 1.97/1.99 2.118 0 Me He 毗咯基 2.119 0 Me Me 2-U-裉咯烷基) 乙基 2.120 0 Me He 2-氟苄基 81-83¾ 2.121 0 Me Me 4-氟苄基 116-118¾2.101 0 Me Me 3-phenylpropyl 2.102 0 Me Me 2- (4-nitrophenyl) ethyl 2.103 0 Me Me 2- (2-CF3-phenyl) ethyl 2.104 0 Me Me 2- (4 -Methylphenyl) ethyl 2.105 0 Me Me 2-chloro-6-fluorobenzyl 2.106 0 He He 3,4 -methinedioxybenzyl 2.107 0 Me Me 2-cyanobenzyl 2.108 0 Me Me 2- (4-azaphenyl) ethyl 2.109 η Me Me Cyanopropylmethyl 1.98 / 1.98 2.110 0 Me Me 2- (1,3-dioxenyl) methyl 2.111 0 Me Me 2, 2 , 3, 3, -tetrafluorobutanyl methyl 2.112 0 Me Me Msstsf —J * -ΛΛ- yuj ot ethoxy * glass methyl 2.113 0 He 2-thipanyl Me 83-86 Ό 2.114 0 Me 4-methyl Base Et 9 4-9 6 TC Phenyl-61- This paper scale is applicable to China National Standard (CNS) Α4 specifications (210X 297mm) (please read the precautions on the back before filling this page) ----- ^ I installed ------ order ----- ^-^ A7 B7 V. Description of the invention (0) Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 2.115 NNe Me 4 -methyl Me Phenyl 2.116 0 Me Me CH2 FCHZ 6 2-6 3 TC 2.117 0 Me Me 2- (4-? Porphyrinyl) ethyl 1.97 / 1.99 2.118 0 Me He pyrrolyl 2.119 0 Me Me 2-U-Pyrrolidinyl) ethyl 2.120 0 Me He 2-fluorobenzyl 81-83¾ 2.121 0 Me Me 4-fluorobenzyl Base 116-118¾

.1 NMe Me Me 6-CF3 -2 - [ft淀基 .2 NMe H Me 6-CF3 -2 - ®i淀基 .3 NNe Me Δ 6-CF3 τ 2 - Ht鹿基 .4 NMe Me H 苯基 .5 NHe Me He 苯基 .6 NMe △ Me 苯基 .7 NHe Me He 4-CF3 -2-吡啶基 .8 NMe H Me 4-CF3 -2-吡啶基 .9 NMe Δ Δ 苯基 -62- (請先閱讀背面之注意事項再填寫本頁) v^f^i nn UK— mu n^i ml Bm n·—· ^^^^1 ί ^^^^1 s n^i ms , - f 洚 i 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央標準局員工消費合作社印製 304860 a? B7 五、發明説明(女η) 3.10 NMe Me He 5-CF3 -2-¾啶基 3.11 NMe H Me 5-CF3 -2 - Bt症基 3.12 -- H Me 4-(1,2 ,4-三唑基) 3.13 -- NMe Me 4- (1 , 2,4-三唑基) 3.14 -- He △ 4-(1,2 ,4-三唑基) 3.15 -- Me Δ 4-嗎啉 基 3.16 -- He Me 4-_啉基 3.17 -- H Me 4-嗎啉基 3.18 HPh* H Me 苯基 3.19 NPh* Me Me 苯基 135-136¾ 3.20 HPh* Me △ 苯基 3.21 NPh* △ Me 苯基 3.22 NMe Me Me 2-硝基苯基 3.23 NMe H Me 2-硝基 苯基 3.24 0 He Me Me 9 0 - 92 1C 3.25 0 H Me Me 1.97/7.68 3.26 0 Δ Me Me 1.94/1.95 3.27 0 Me Δ He 88- 9 0 t! 3.28 0 Me H Me 3.29 NMe H Me 3-CF3 -2-吡啶基 3.30 NMe Me Me 3-CF3 -2-吡啶基 3.31 NMe △ Me 3-CF3 -2-吡啶基 3.32 NMe Δ Me 3-硝基 -2-吡啶基 _ 6 3 _ ; ^ -裝 i (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(θ ) A7 B7 經濟部中央標準局員工消費合作社印製 3.33 NMe H Me 3-硝基-2-¾啶基 3.34 NMe Me Me 3-硝基-2-¾啶基 3.35 NMe Me Me 2-CF3 -苯基 3.36 NMe Me △ 2-CF3 -苯基 3.37 NMe H Me 2-CF3 -苯基 3.38 NMe He Me 3-C F3 -苯基 3.39 NNe Me Δ 3-CFs _苯基 3.40 NMe H He 4-CF3 -苯基 3.41 NHe Me Me 4-CF3 -苯基 3.42 NMe Me Me 2-氰苯基 1.72/2.11 3.43 NHe Me He 3-氛苯基 2.09/2.14 3.44 NHe H Me 4-氣苯基 3.45 NMe Me Me 4-氩苯基 2.08/2.13 3.46 0 Me He 苯基 3.47 0 Me △ 苯基 3.48 0 He Me 苄基 3.49 0 Me He Et 3.50 0 H Me Et 3.51 0 △ Me Et 3.52 0 Me Δ Et 3.53 0 Me H Et 3.54 0 H Me 甲氣基甲基 3.55 0 Me Me 甲氣基甲基 2.00/2.03 一 6 4 _ (請先閱讀背面之注意事項再填寫本頁) ^^^1 ^^^1 n^( ^^^1 n^l HI n^— ^^^1 ^1^1 ^^^1 1^^1 1^^1 mj' I ml ^in n^i nn ·ϋι ^ϋ 一 V ^^^1 ml n^i fl^i 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(矽) A7 B7 經濟部中央標準局員工消費合作社印製 3.56 0 Me Δ 甲氣基甲基 3.57 0 △ He 甲氣基甲基 3.58 0 He Me 乙氣基甲基 3.59 0 Me Me 氣基甲基 3.60 0 He Me 氱基甲基 2.00/2.01 3.61 - Δ Me 氱基甲基 3.62 - Me Me 氮雜蘿基 3.63 - Me Me 锹啶烷基 3.64 0 Me Me 吡啶烷基 3.65 0 H He 三级丁基 3.66 0 Me Me 三级丁基 1.95/2.01 3.67 0 Me Me 炔丙基 114-115¾ 3.68 0 Δ He 炔丙基 3.69 0 Me Δ 炔丙基 3.70 0 Me Me 2 , 2-二氯琛 1.99/1.99 丙基甲基 3.71 0 △ Me 2, 2-二氯環 丙基甲基 3.72 0 Me Me Η 3.73 0 Me Me Η 3.74 0 Me Me CF3 CHz 94- 9 6 t: 3.75 0 △ Me CF3 CHz 3.76 0 Me H CF3 CHz -65- (請先閲讀背面之注意事項再填寫本頁) ^^^1 ^^^1 nn n^i m n^— nn i n^i 1^1 nn urn— nn ^^^1 ^ J. n^^i In ^^^1 &gt;^v. · &gt;3^* . . ^ 0¾. 、\=tl-4期 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 304860 五、發明説明U。) A7 B7 經濟部中央標準局員工消費合作社印製 3.77 0 Me H cf3 ch2 ch2 3.78 0 Me Me CF3 CHz CH2 3.79 0 Me Me cf3 ch2 ch2 ch2 3.80 0 Δ Me CF3 CHz CH2 CHz 3.81 0 NMe Me Me 90-9 It: 3.82 0 NNe Δ He 3.83 0 Me Me CH2 -CC1 = CHz 1.97/2.02 3.84 0 △ Me CH2 -CC1 = CH2 3.85 0 Me He 丙基 3.86 0 Me Me 丁基 9 1-92¾ 3.87 0 Me Me 己基 84 -86 ¾ 3.88 0 Me Me 甲氣基羰基甲基 1 2 7 - 1 2 9 t: 3.89 0 H He 甲氣基羰基甲基 3.90 0 Me He 3-氟苄基 3.91 0 Me Me 4-氯苄基 3.92 0 Me He 2-氛苄基 3.93 0 Me Me 2-CF3 -苄基 3.94 0 Me Me 3-CF3 -苄基 1.96/2.00 3.95 0 Me Me 4-CF3 -苄基 3.96 0 Me Me 3,4-二氱苄基 3.97 0 Me Me 2 ,4 , 6-三 甲基苄基 3.98 0 Me Me 4-氯-2-硝基苄基 3.99 0 Me Me 3-甲氣基苄基 -66- (請先閱讀背面之注意事項再填寫本頁) --·------^ 丨裝------訂-----線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(έ丨) 3.100 0 Me Me 2-苯基丙基 3.101 0 He He 3-苯基丙基 3.102 0 Me He 2-(4-硝基苯 基)乙基 3.103 0 He Me 2- (2-CF3 -苯基) 乙基 3.104 0 Me Me 2-(4-甲氣基苯 基)乙基 3.105 0 Me Me 2-氛-6-氟苄基 3.106 0 Me Me 3,4-次甲基二 氣基苄基 3.107 0 Me Me 2-気基苄基 3.108 0 Me Me 2- (4-氯苯基)乙基 3.109 0 Me Me 氱基丙基甲基 2.00/2.00 3.110 0 Me Me 2-(1 , 3-二噁茂 基)甲基 3.111 0 Me Me 2 , 2 , 3 , 3 ,-四氟環 丁基甲基 3.112 0 Me Me α -氟乙氣基羰 基甲基 3.113 0 Me 2-唾吩基 Me 3.114 0 Me 4-甲基 Et 1 0 3 - 1 04 ¾ -67- (請先閲讀背面之注意事項再填寫本頁) ---f'丨裝------訂-----f' 線 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) A7 B7 五、發明説明(h) 苯基.1 NMe Me Me 6-CF3 -2-[ft Dianji. 2 NMe H Me 6-CF3 -2-®i Dianji. 3 NNe Me Δ 6-CF3 τ 2-Ht deeryl. 4 NMe Me H Benzene Base. 5 NHe Me He phenyl. 6 NMe △ Me phenyl. 7 NHe Me He 4-CF3 -2-pyridyl. 8 NMe H Me 4-CF3 -2-pyridyl. 9 NMe Δ Δ phenyl-62 -(Please read the precautions on the back before filling out this page) v ^ f ^ i nn UK— mu n ^ i ml Bm n · — · ^^^^ 1 ί ^^^^ 1 sn ^ i ms,-f洚 i line paper size is applicable to China National Standards (CNS) A4 (210X297mm) Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 304860 a? B7 V. Invention description (female η) 3.10 NMe Me He 5-CF3- 2-¾-Pyridyl 3.11 NMe H Me 5-CF3 -2-Bt Syndrome 3.12-H Me 4- (1,2, 4-triazolyl) 3.13-NMe Me 4- (1, 2,4- Triazolyl) 3.14-He △ 4- (1,2,4-triazolyl) 3.15-Me Δ 4-morpholinyl 3.16-He Me 4-_morpholinyl 3.17-H Me 4- Porphyrinyl 3.18 HPh * H Me Phenyl 3.19 NPh * Me Me Phenyl 135-136¾ 3.20 HPh * Me △ Phenyl 3.21 NPh * △ Me Phenyl 3.22 NMe Me Me 2-Nitrophenyl 3.23 NMe H Me 2- Phenyl 3.24 0 He Me Me 9 0-92 1C 3.25 0 H Me Me 1.97 / 7.68 3.26 0 Δ Me Me 1.94 / 1.95 3.27 0 Me Δ He 88- 9 0 t! 3.28 0 Me H Me 3.29 NMe H Me 3 -CF3 -2-pyridyl 3.30 NMe Me Me 3-CF3 -2-pyridyl 3.31 NMe △ Me 3-CF3 -2-pyridyl 3.32 NMe Δ Me 3-nitro-2-pyridyl _ 6 3 _; ^ -Install i (Please read the precautions on the back before filling in this page) This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) V. Invention description (θ) A7 B7 Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Print 3.33 NMe H Me 3-nitro-2-¾-pyridyl 3.34 NMe Me Me 3-nitro-2-¾-pyridyl 3.35 NMe Me Me 2-CF3-phenyl 3.36 NMe Me △ 2-CF3-phenyl 3.37 NMe H Me 2-CF3 -phenyl 3.38 NMe He Me 3-C F3 -phenyl 3.39 NNe Me Δ 3-CFs _phenyl 3.40 NMe H He 4-CF3 -phenyl 3.41 NHe Me Me 4-CF3 -benzene Base 3.42 NMe Me Me 2-cyanophenyl 1.72 / 2.11 3.43 NHe Me He 3-aminophenyl 2.09 / 2.14 3.44 NHe H Me 4-gas phenyl 3.45 NMe Me Me 4-argylphenyl 2.08 / 2.13 3.46 0 Me He Phenyl 3.47 0 Me △ Phenyl 3.48 0 He Me Benzyl 3.49 0 Me He Et 3.50 0 H Me Et 3.51 0 △ Me Et 3.52 0 Me Δ Et 3.53 0 Me H Et 3.54 0 H Me Methylmethyl 3.55 0 Me Me Methylmethyl 2.00 /2.03 1 6 4 _ (Please read the precautions on the back before filling out this page) ^^^ 1 ^^^ 1 n ^ (^^^ 1 n ^ l HI n ^ — ^^^ 1 ^ 1 ^ 1 ^ ^^ 1 1 ^^ 1 1 ^^ 1 mj 'I ml ^ in n ^ i nn · ϋι ^ ϋ a V ^^^ 1 ml n ^ i fl ^ i This paper scale is applicable to the Chinese National Standard (CNS) A4 specifications (210X297mm) V. Description of invention (silicon) A7 B7 Printed by the Employees ’Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 3.56 0 Me Δ Methylmethyl 3.57 0 △ He Methylmethyl 3.58 0 He Me Base 3.59 0 Me Me Aminomethyl 3.60 0 He Me Trimethyl 2.00 / 2.01 3.61-Δ Me Trimethyl 3.62-Me Me Azalyl 3.63-Me Me Dipyridyl 3.64 0 Me Me Pyridine Base 3.65 0 H He tertiary butyl 3.66 0 Me Me tertiary butyl 1.95 / 2.01 3.67 0 Me Me propargyl 114-115¾ 3.68 0 Δ He propargyl 3.69 0 Me Δ propargyl 3.70 0 Me Me 2, 2-Dichlorohydrazine 1.99 / 1.99 Propyl methyl 3.71 0 △ Me 2, 2-dichlorocyclopropylmethyl 3.72 0 Me Me Η 3.73 0 Me Me Η 3.74 0 Me Me CF3 CHz 94- 9 6 t: 3.75 0 △ Me CF3 CHz 3.76 0 Me H CF3 CHz -65 -(Please read the notes on the back before filling out this page) ^^^ 1 ^^^ 1 nn n ^ imn ^ — nn in ^ i 1 ^ 1 nn urn— nn ^^^ 1 ^ J. n ^^ i In ^^^ 1 &gt; ^ v. · &Gt; 3 ^ *.. ^ 0¾., \ = Tl-4 This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 304860 V. Description of invention U. ) A7 B7 Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 3.77 0 Me H cf3 ch2 ch2 3.78 0 Me Me CF3 CHz CH2 3.79 0 Me Me cf3 ch2 ch2 ch2 3.80 0 Δ Me CF3 CHz CH2 CHz 3.81 0 NMe Me Me 90- 9 It: 3.82 0 NNe Δ He 3.83 0 Me Me CH2 -CC1 = CHz 1.97 / 2.02 3.84 0 △ Me CH2 -CC1 = CH2 3.85 0 Me He propyl 3.86 0 Me Me Butyl 9 1-92¾ 3.87 0 Me Me hexyl 84 -86 ¾ 3.88 0 Me Me Methoxycarbonylmethyl 1 2 7-1 2 9 t: 3.89 0 H He Methoxycarbonylmethyl 3.90 0 Me He 3-fluorobenzyl 3.91 0 Me Me 4-chlorobenzyl Base 3.92 0 Me He 2-aminobenzyl 3.93 0 Me Me 2-CF3 -benzyl 3.94 0 Me Me 3-CF3 -benzyl 1.96 / 2.00 3.95 0 Me Me 4-CF3 -benzyl 3.96 0 Me Me 3,4 -Dipropylbenzyl 3.97 0 Me Me 2, 4, 6-trimethylbenzyl 3.98 0 Me Me 4-chloro-2-nitrobenzyl 3.99 0 Me Me 3-methoxybenzyl-66- (please Read the precautions on the back first and then fill out this page)-· ------ ^ 丨 installed ------ ordered ----- The size of the line paper is applicable to the Chinese National Standard (CNS) A4 specification (210X297 Mm) Employee consumption of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the cooperative A7 B7 5. Description of the invention (έ 丨) 3.100 0 Me Me 2-phenylpropyl 3.101 0 He He 3-phenylpropyl 3.102 0 Me He 2- (4-nitrophenyl) ethyl 3.103 0 He Me 2- (2-CF3-phenyl) ethyl 3.104 0 Me Me 2- (4-methylphenyl) ethyl 3.105 0 Me Me 2-ambient-6-fluorobenzyl 3.106 0 Me Me 3 , 4-Methylenedioxybenzyl 3.107 0 Me Me 2- 気 benzyl 3.108 0 Me Me 2- (4-chlorophenyl) ethyl 3.109 0 Me Me propylpropylmethyl 2.00 / 2.00 3.110 0 Me Me 2- (1, 3-dioxenyl) methyl 3.111 0 Me Me 2, 2, 3, 3, -tetrafluorocyclobutylmethyl 3.112 0 Me Me α -fluoroethoxycarbonylmethyl 3.113 0 Me 2-Sialenyl Me 3.114 0 Me 4-methyl Et 1 0 3-1 04 ¾ -67- (please read the precautions on the back before filling this page) --- f '丨 install ------ Order ----- f 'line paper size is applicable to China National Standard (CNS) Α4 specification (210X297mm) A7 B7 5. Description of invention (h) Phenyl

3.115 NHe Me 4-甲基 Me 9 5- 9 7 ^ 苯基 3.116 0 Me Me ch2 fch2 95 - 9 7 ¾ 3.117 0 Me Me 2-(4-嗎啉基)乙基 1.98/2.06 3.118 0 Me He 吡咯基 3.119 0 Me Me 2-(1-哌咯烷基) 1.96/1.98 乙基 3.120 0 Me Me 2-氟苄基 90-91 Ό 3.121 0 Me Me 4-氰苄基 130-131¾ 窣# R 1 /Rz 或R3 的 . p .或1 H NMR -------·------^ I 裝------訂-----^ --^ (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 本紙張尺度逋用中國國家標準(CNS ) A4規格(210X297公釐) 304860 經濟部中央揉率局負工消费合作社印製 -ί ί . A7 B73.115 NHe Me 4-methyl Me 9 5- 9 7 ^ phenyl 3.116 0 Me Me ch2 fch2 95-9 7 ¾ 3.117 0 Me Me 2- (4-morpholinyl) ethyl 1.98 / 2.06 3.118 0 Me He pyrrole Base 3.119 0 Me Me 2- (1-piperolidinyl) 1.96 / 1.98 ethyl 3.120 0 Me Me 2-fluorobenzyl 90-91 Ό 3.121 0 Me Me 4-cyanobenzyl 130-131¾ 窣 # R 1 / Rz or R3. P. Or 1 H NMR ------- · ------ ^ I loaded ------ ordered ----- ^-^ (please read the back of it first (Notes to fill out this page) Printed paper size of the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs is printed in Chinese National Standard (CNS) A4 (210X297mm) ί. A7 B7

實例 X Y R i Z* n B或D 物理資料 編號 幸《 4.1 CH OMe Me - 1 3-CF3 1 3 3 - 1 3 5 ¾ 4.2 CH ONe Me - 1 4-氣 1 4 0 - 1 4 2 Ϊ: 4 . 3 CH OMe Ke - 1 3-氮 175- 177 ¾ 4.4 CH OMe Me - 1 2-氟 1 3 6- 1 3 7*0 4.5 CH OMe Me - 1 4-甲基 異構物1. 98-l〇nD 異構物2.油 異構物3.油 4.6 CH OMe Me 0 0 甲基- 104-106¾ 4.7 CH OMe Me - 1 4-溴 126-128¾ 4.8 CH OMe Me - 1 4-氣 14 1- 144 t: 4.9 CH OMe Me - 2 3-氰-5-CF3 1 64 - 1 6 6 10 4.10 CH OHe Me - 0 __ 141- 143υ _ 6 9 _ (請先閲讀背面之注意事項再填寫本頁) 裝· -·· 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明Ut) A7 B7 經濟部中央揲率局員工消費合作社印裝 4.11 CH OMe Me - 1 2-甲基 113-U5t: 4.12 CH OMe Me - 1 3-溴 176-178¾ 4.13 CH OMe Me - 2 3,4-次甲 1 4 3- 1 4 5 ¾ 基二氣基 4.14 CH OMe Me 0 0 烯丙基- 7 7-80 t:(異構物 2.08(異構物2) 4.15 CH OMe SMe - 1 4-甲基 2.08(異構物1) 2. 11(異構物2) 4.16 CH OMe E t - 1 4-甲基 3.90(異構物1) 3.97(異構物2) 4.17 CH OMe Me - 1 4-異丁基- 2. 11(異構物1) 2.08(異構物2) 4.18 CH OMe Me 0 0 丙烯基 2.06/2.11 (E/Z) 4.19 CH OMe He 0 0 2,2,2-三氟 2. 11(異構物1) 乙基 2.07(異構物2) 4.20 CH OMe Me 0 0 乙基 9 3 - 95 C (異構物 2.06(異構物2) 4.21 CH OMe CN - 1 4-甲基 98-133¾ (E/Z) 4.22 CH OMe CN - 1 4-氣 106-108¾ 4.23 CH OMe CN - 2 3,4-二氛 1 2 8- 1 3 0 t: 1 0 9-1111: (E/Z) 4.24 CH OMe CN 0 0 -CFs 油(E/Z) 4.25 CH OMe CN - 1 3-CF3 -70- ^ 1 裝 訂 ^線 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) A7 B7 五、發明説明U_r) 經濟部中央揉準局員工消費合作社印製 4.26 CH OHe CN - 1 2-氯 4.27 CH OMe CN - 1 4-氟 4.28 CH OMe Me 0 0 苯基 112-U41C (異構物 油(異構物2) 4.29 CH OHe Me 0 0 -CHZ CH=CClz 4.30 CH OMe Me 0 0 ch2 ch=cf2 4.31 CH OMe Me 0 0 -CHz CH=CBrz 4.32 CH OMe Me 0 0 4-氯-苯基 4.33 CH OMe He 0 0 4-氟-苯基 4.34 CH OHe Me s 0 苯基 4.35 CH OMe Me ch2 0-0 苯基 異構物1:樹脂 異構物2 :樹脂 4.36 CH OHe Me CHe 0-1 苯基 油 4.37 N ONe Me - 1 3-CF3 4.38 N OMe Me - 1 4-氛 4.39 N OMe Me - 1 3-氰 4.40 N OMe Me - 1 2-覦 lll-112t: 4.41 Η OMe Me - 1 4-甲基 101-103¾ 4.42 Ν OHe Me 0 0 4-甲基- 1 0 4 - 1 0 6 ¾ 4.43 Ν OHe Me - 1 4-溴 1 3 4- 1 3 6 Ό 4.44 Ν OMe Me - 1 4-氟 4.45 Ν OHe Me - 2 3-F-5-CF3 4.46 Ν OMe Me - 0 - -71- (¾先閱讀背面之注意事項再填寫本頁) .裝. 訂 -線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(0 ) A7 B7 經濟部中央標準局員工消費合作社印製 t «/» 4.47 N OHe Me - 1 2-甲基 1 05- 1 0 7 1C 4.48 N OMe Me - 1 3-溴 4.49 N OMe Me - 2 3,4-次甲基二氣 4.50 N OMe Me 0 0 烯丙基 74 - 7 6 10 4.51 N OMe SHe - 1 4-甲基 88-9η〇 4.52 N OMe Et - 1 4-甲基 4.53 N OMe Me - 1 4-異丁基- 4.54 N OMe Me 0 0 丙烯基 油 4 .55 N OHe Me 0 0 2 , 2, 2-三氟乙基 4.56 N OHe Me 0 0 乙基 油 4.57 N OMe CN - 1 4-甲基 4.58 N OMe CN - 1 4-氰 4.59 N OMe CN - 2 3.4-二氯 4.60 N OMe CN 0 0 -CFs 4.61 N OMe CN - 1 3-CF3 4.62 N OMe CN - 1 2-氯 4.63 N OHe CN - 1 4-氟 4.64 N OMe Ne 0 0 苯基 4.65 N OMe Me 0 0 -ch2 ch=ci2 4.66 N OMe Me 0 0 ch2 ch=cf2 4.67 N OMe Me 0 0 -CH2 CH=CBr2 4.68 N OHe Me 0 0 4-氣-苯基 4.69 N OMe Me 0 0 4-氟-苯基 -72- (請先閱讀背面之注意事項再填寫本頁) ^^^^1 ^^^^1 ^^^^1 ^^i·—· mV ^^^^1 1^^1 ^in n·^— — —^n ^^tmrm I 1 ml nn .^m ^^^^1 B1 I . · J 、1 7 期 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(θ) A7 B7 經濟部中央標準局員工消費合作社印製 « ·· · 4.I071N N ONINe NeMeSCHz 0- 笨基基*»» 4.72 N OHe Me OCHz -0 苯基》** 4.73 N HHCHs He - 1 3-CF3 4.74 N NHCH3 Me - 1 4-氱 4.75 N NHCHa Me - 1 3-氛 4.76 N nhch3 Me - 1 2-氟 2.11 4.77 N nhch3 Me - 1 4-甲基 2.10 4.78 N NHCH3 Me 0 0 甲基- 4.79 N NHCH3 Me 1 4-溴 2.09 4 .80 N NHCH3 Me - 1 4-瓤 4.81 N nhch3 Ke - 2 3-F-5-CF3 4.82 N nhch3 Me - 0 - 4.83 N NHCHa Me - 1 2-甲基 2.05 4.84 N NHCH3 Me - 1 3-溴 4.85 N NHCH3 Me - 2 3,4-次甲基 二 氣基 4.86 N NHCH3 Me 0 0 烯丙基 118-120¾ 4.87 N NHCH3 SMe - 1 4-甲基 2.06 4.88 N NHCH3 Et - 1 4-甲基 4.89 N nhch3 Me - 1 4-異丁基- 4.90 N NHCH3 Me 0 0 丙烯基 油 4.91 N NHCH3 Me 0 0 2,2,2-三概乙基 -73- I ,, ( I裝 訂 ^線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 304860 五、發明説明(“) A7 B7 經濟部中央標準局員工消費合作社印製 4.92 N NHCH3 Me 0 0 乙基 油 4.93 N NHCH3 CN - 1 4-甲基 4.94 N NHCH3 CN - 1 4-氨 4.95 N NHCH3 CN - 1 3,4-二氯 4.96 N NHCH3 CN 0 0 -cf3 4.97 N NHCH3 CN - 1 3-CF3 4 .98 N NHCH3 CN - 1 2-« 4.99 N NHCH3 CN - 1 4-氟 4.100 N NHCH3 Me 0 0 苯基 4.101 N NHCH3 Me 0 0 -CHZ &amp; He 0 0 ch2 ch= 4.103 N NHCH3 Me 0 0 -CH2 CH=CBr2 4.104 N NHCH3 Me 0 0 4-氯-苯基 4.105 N NHCH3 Me 0 0 4-氟-苯基 4.106 N NHCH3 Me s 0 苯基 4.107 N NKCH3 Me -ch2 00 苯基 4.108 N NHCH3 He 0CH2 0 苯基 * $窣 4.109 CH 0CH3 Me 0 0 正丙基 異構物1:油 異構物2 :油 4.110 CH 0CH3 Me 0 0 3 , 3-二甲基 丙烯基 107-110t:(異構物 油(異構物2) 4.111 CH OCH3 Me 0 0 2-甲基- 烯丙基 -74- 異構物1 : 9 7 - 9 9 t: 異構物2:油 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐〉 A7 B7 五、發明説明(6?) 經濟部中央標準局員工消費合作社印製 4.112 CH 0CH3 Me 0 0 3 -甲基- 異構物1:油 烯丙基 4.113 CH 0 ch3 Me 0 0 烯丙基 異構物1 : 7 4 - 7 6 1C 4.114 CH 0CH3 Me 0 0 丙烯基 油 4.115 CH NHCH3 Me 0 0 烯丙基 4.116 CH NHCH3 Me 0 0 丙烯基 4.117 CH OCH3 Me 0CH2 -0 3-CF3 -苯基 異構物1:83-85¾ « « « 異構物1 :樹脂 4.118 CH OCH3 Me 0 0 3-CF3 -苯基 異構物1 : 127-128 異構物2:油 4.119 CH OCH3 Me OCHz -0 C6 Η 1 1 *** 異構物1:油 異携物2:油 4.120 CH OCH3 Me 0CH2 -0 苯基*** 異構物1:油 異構物2 :油 4.121 CH OCH3 Me OCHz -0 4-F-苯基 異構物1:油 « « « 異構物2:油 4.122 CH OCH3 Me s 0 CH3 異構物1 : 119-121 異構物2:樹脂 4.123 CH OCH3 Me -S〇2 -0 ch3 異構物1:泡沫 異構物2 :樹脂 4.124 CH OCH3 Me OCHz -0 苯基*㈣ 異構物1:油 異構物2 :樹脂 4.125 CH OCH3 He OCHz -0 4-CF3 V -75- ---7------f Ί-- (請先閲讀背面之注意事項再填寫本頁) ,νβ &quot; 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 五、發明説明(γ) A7 B7 經濟部中央標準局員工消費合作社印製 4.126 CH 0CH3 He OCHz -0 4-溴-苯基*»* 4.127 CH 0CH3 Me OCHz -0 4-CH3 -苯基 *** 4.128 CH 0CH3 Me OCHz -0 4-0CH3 -苯基 *** 4.129 CH OCH3 Me 0CH2 -0 2-CF3 -苯基 *** 4.130 CH OCH3 Me OCHz -0 2-F-苯基 *** 異構物1:油 異構物2:油 4.131 CH OCH3 Me 0CH2 -0 2-C1-苯基*㈣ 4.132 CH OCH3 Me OCHz -0 2- Br-3f 16 *** 4.133 CH OCH3 Me OCH2 -0 3-F-苯基 異構物1: 111-112 異構物2 :油 4.134 CH OCH3 Me OCH2 -0 3-C1-苯基 異構物1:油 異構物2:油 4.135 CH OCH3 Me OCHz -0 3-溴-苯基 異構物1 :樹脂 異構物2 : Harz 4.136 Ν OCH3 Me 0CH2 -0 烯丙基 4.137 Ν OCH3 Me OCHz -0 3-CF3 -苯基 ** 4.138 Ν OCH3 Me OCHz -0 3-CF3 -苯基 *** 4.139 Ν OCH3 Me - 1 2-CF3 油 4.140 Ν OCH3 Me - 1 2-CH3 異嫌物1 : 105-107 異構物2 :樹脂 4.141 Ν NHCH3 Me - 1 2-CF3 樹脂 4.142 Ν NHCH3 Me - 1 2-CH3 異構物1:油 異構物2:油 一 7 6 _ --7------·裝-- (請先閱讀背面之注意事項再填寫本頁) C 本紙張尺度逋用中國國家標準(CNS ) Α4規格(210Χ297公釐)Example XYR i Z * n B or D Physical data number Xing "4.1 CH OMe Me-1 3-CF3 1 3 3-1 3 5 ¾ 4.2 CH ONe Me-1 4-gas 1 4 0-1 4 2 Ϊ: 4 . 3 CH OMe Ke-1 3-nitrogen 175- 177 ¾ 4.4 CH OMe Me-1 2-fluoro1 3 6- 1 3 7 * 0 4.5 CH OMe Me-1 4-methyl isomer 1. 98-l 〇nD isomer 2. Oil isomer 3. Oil 4.6 CH OMe Me 0 0 Methyl-104-106¾ 4.7 CH OMe Me-1 4-bromo 126-128¾ 4.8 CH OMe Me-1 4-gas 14 1- 144 t: 4.9 CH OMe Me-2 3-cyano-5-CF3 1 64-1 6 6 10 4.10 CH OHe Me-0 __ 141- 143υ _ 6 9 _ (please read the notes on the back before filling this page) Installation ·-·· This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) V. Description of invention Ut) A7 B7 Printed by the Employees Consumer Cooperative of the Central Bureau of Economic Affairs of the Ministry of Economic Affairs 4.11 CH OMe Me-1 2-A Radix 113-U5t: 4.12 CH OMe Me-1 3-bromo 176-178¾ 4.13 CH OMe Me-2 3,4-methylene 1 4 3- 1 4 5 ¾ Dioxo 4.14 CH OMe Me 0 0 allyl -7 7-80 t: (isomer 2.08 (isomer 2) 4.15 CH OMe SMe-1 4-methyl 2.08 (Isomer 1) 2. 11 (Isomer 2) 4.16 CH OMe E t-1 4-methyl 3.90 (Isomer 1) 3.97 (Isomer 2) 4.17 CH OMe Me-1 4-isobutyl Group-2.11 (isomer 1) 2.08 (isomer 2) 4.18 CH OMe Me 0 0 propenyl 2.06 / 2.11 (E / Z) 4.19 CH OMe He 0 0 2,2,2-trifluoro 2. 11 (isomer 1) ethyl 2.07 (isomer 2) 4.20 CH OMe Me 0 0 ethyl 9 3-95 C (isomer 2.06 (isomer 2) 4.21 CH OMe CN-1 4-methyl 98-133¾ (E / Z) 4.22 CH OMe CN-1 4-gas 106-108¾ 4.23 CH OMe CN-2 3,4-diamine 1 2 8- 1 3 0 t: 1 0 9-1111: (E / Z Z) 4.24 CH OMe CN 0 0 -CFs oil (E / Z) 4.25 CH OMe CN-1 3-CF3 -70- ^ 1 binding ^ line (please read the precautions on the back before filling this page) This paper size is applicable China National Standard (CNS) Α4 specification (210Χ297mm) A7 B7 V. Description of the invention U_r) Printed by the Ministry of Economic Affairs Central Bureau of Standards and Staff ’s Consumer Cooperatives 4.26 CH OHe CN-1 2-chloro 4.27 CH OMe CN-1 4-fluoro 4.28 CH OMe Me 0 0 Phenyl 112-U41C (isomer oil (isomer 2) 4.29 CH OHe Me 0 0 -CHZ CH = CClz 4 .30 CH OMe Me 0 0 ch2 ch = cf2 4.31 CH OMe Me 0 0 -CHz CH = CBrz 4.32 CH OMe Me 0 0 4-chloro-phenyl 4.33 CH OMe He 0 0 4-fluoro-phenyl 4.34 CH OHe Me s 0 phenyl 4.35 CH OMe Me ch2 0-0 phenyl isomer 1: resin isomer 2: resin 4.36 CH OHe Me CHe 0-1 phenyl oil 4.37 N ONe Me-1 3-CF3 4.38 N OMe Me -1 4-atmosphere 4.39 N OMe Me-1 3-cyano 4.40 N OMe Me-1 2- 觎 lll-112t: 4.41 Η OMe Me-1 4-methyl 101-103¾ 4.42 Ν OHe Me 0 0 4-methyl -1 0 4-1 0 6 ¾ 4.43 Ν OHe Me-1 4-bromo1 3 4- 1 3 6 Ό 4.44 Ν OMe Me-1 4-fluoro 4.45 Ν OHe Me-2 3-F-5-CF3 4.46 Ν OMe Me-0--71- (¾ Read the precautions on the back before filling out this page). Binding. Binding-The size of the paper is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) V. Description of invention (0 ) A7 B7 Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs «/» 4.47 N OHe Me-1 2-methyl 1 05- 1 0 7 1C 4.48 N OMe Me-1 3-bromo 4.49 N OMe Me-2 3 , 4-Methylene Digas 4.50 N OMe Me 0 0 Allyl 74-7 6 10 4.51 N OMe SHe- 1 4-methyl 88-9η〇4.52 N OMe Et-1 4-methyl 4.53 N OMe Me-1 4-isobutyl- 4.54 N OMe Me 0 0 propylene-based oil 4.55 N OHe Me 0 0 2, 2, 2-trifluoroethyl 4.56 N OHe Me 0 0 ethyl oil 4.57 N OMe CN-1 4-methyl 4.58 N OMe CN-1 4-cyano 4.59 N OMe CN-2 3.4-dichloro 4.60 N OMe CN 0 0 -CFs 4.61 N OMe CN-1 3-CF3 4.62 N OMe CN-1 2-chloro 4.63 N OHe CN-1 4-fluoro 4.64 N OMe Ne 0 0 phenyl 4.65 N OMe Me 0 0 -ch2 ch = ci2 4.66 N OMe Me 0 0 ch2 ch = cf2 4.67 N OMe Me 0 0 -CH2 CH = CBr2 4.68 N OMe Me 0 0 4-gas-phenyl 4.69 N OMe Me 0 0 4-fluoro-phenyl-72- (please Read the notes on the back before filling out this page) ^^^^ 1 ^^^^ 1 ^^^^ 1 ^^ i · — · mV ^^^^ 1 1 ^^ 1 ^ in n · ^ — — — ^ n ^^ tmrm I 1 ml nn. ^ m ^^^^ 1 B1 I. · J, 17 This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) V. Description of the invention (θ) A7 B7 Printed «··· 4.I071N N ONINe NeMeSCHz 0- Benkiji *» »4.72 N OHe Me OCHz -0 Phenyl》 4.73 N HHC Hs He-1 3-CF3 4.74 N NHCH3 Me-1 4- 氱 4.75 N NHCHa Me-1 3-atmosphere 4.76 N nhch3 Me-1 2-fluoro 2.11 4.77 N nhch3 Me-1 4-methyl 2.10 4.78 N NHCH3 Me 0 0 Methyl- 4.79 N NHCH3 Me 1 4-Bromo 2.09 4 .80 N NHCH3 Me-1 4-Feng 4.81 N nhch3 Ke-2 3-F-5-CF3 4.82 N nhch3 Me-0-4.83 N NHCHa Me- 1 2-methyl 2.05 4.84 N NHCH3 Me-1 3-bromo 4.85 N NHCH3 Me-2 3,4-methylenedioxy 4.86 N NHCH3 Me 0 0 allyl 118-120¾ 4.87 N NHCH3 SMe-1 4 -Methyl 2.06 4.88 N NHCH3 Et-1 4-methyl 4.89 N nhch3 Me-1 4-isobutyl- 4.90 N NHCH3 Me 0 0 propylene-based oil 4.91 N NHCH3 Me 0 0 2,2,2-trifluoroethylene基 -73- I ,, (I binding ^ line (please read the notes on the back before filling in this page) This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 304860 V. Description of invention (“) A7 B7 Printed 4.92 N NHCH3 Me 0 0 ethyl oil 4.93 N NHCH3 CN-1 4-methyl 4.94 N NHCH3 CN-1 4-ammonia 4.95 N NHCH3 CN-1 3,4- Dichloro 4 .96 N NHCH3 CN 0 0 -cf3 4.97 N NHCH3 CN-1 3-CF3 4 .98 N NHCH3 CN-1 2- «4.99 N NHCH3 CN-1 4-fluoro 4.100 N NHCH3 Me 0 0 Phenyl 4.101 N NHCH3 Me 0 0 -CHZ & He 0 0 ch2 ch = 4.103 N NHCH3 Me 0 0 -CH2 CH = CBr2 4.104 N NHCH3 Me 0 0 4-chloro-phenyl 4.105 N NHCH3 Me 0 0 4-fluoro-phenyl 4.106 N NHCH3 Me s 0 phenyl 4.107 N NKCH3 Me -ch2 00 phenyl 4.108 N NHCH3 He 0CH2 0 phenyl * $ 窣 4.109 CH 0CH3 Me 0 0 n-propyl isomer 1: oil isomer 2: oil 4.110 CH 0CH3 Me 0 0 3, 3-dimethylpropenyl 107-110t: (isomer oil (isomer 2) 4.111 CH OCH3 Me 0 0 2-methyl-allyl-74- isomer 1: 9 7 -9 9 t: Isomer 2: Oil (please read the precautions on the back before filling this page) This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) A7 B7 V. Invention description (6? ) Printed by the Employees ’Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 4.112 CH 0CH3 Me 0 0 3 -methyl-isomer 1: oleyl 4.13 CH 0 ch3 Me 0 0 allyl isomer 1: 7 4-7 6 1C 4.114 CH 0CH3 Me 0 0 C Base oil 4.115 CH NHCH3 Me 0 0 allyl 4.116 CH NHCH3 Me 0 0 propenyl 4.117 CH OCH3 Me 0CH2 -0 3-CF3 -phenyl isomer 1: 83-85¾ «« «Isomer 1: Resin 4.118 CH OCH3 Me 0 0 3-CF3 -phenyl isomer 1: 127-128 Isomer 2: oil 4.119 CH OCH3 Me OCHz -0 C6 Η 1 1 *** Isomer 1: oil isomer 2: Oil 4.120 CH OCH3 Me 0CH2 -0 Phenyl *** Isomer 1: Oil Isomer 2: Oil 4.121 CH OCH3 Me OCHz -0 4-F-Phenyl Isomer 1: Oil «« «Isomer 2: Oil 4.122 CH OCH3 Me s 0 CH3 Isomer 1: 119-121 Isomer 2: Resin 4.123 CH OCH3 Me -S〇2 -0 ch3 Isomer 1: Foam Isomer 2: Resin 4.124 CH OCH3 Me OCHz -0 Phenyl * (iv) Isomer 1: Oil isomer 2: Resin 4.125 CH OCH3 He OCHz -0 4-CF3 V -75- --- 7 ------ f Ί-- (Please Read the precautions on the back and then fill out this page), νβ &quot; This paper standard is applicable to the Chinese National Standard (CNS) Α4 specification (210Χ297mm) V. Description of invention (γ) A7 B7 Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Control 4.126 CH 0CH3 He OCHz -0 4-bromo-phenyl * »* 4.127 CH 0CH3 Me OCHz -0 4-CH3 -phenyl *** 4.128 CH 0CH3 Me OCHz -0 4-0CH3 -phenyl *** 4.129 CH OCH3 Me 0CH2 -0 2-CF3 -phenyl *** 4.130 CH OCH3 Me OCHz -0 2-F-phenyl *** Isomer 1: oil isomer 2: oil 4.131 CH OCH3 Me 0CH2 -0 2 -C1-Phenyl * (4.132 CH OCH3 Me OCHz -0 2- Br-3f 16 *** 4.133 CH OCH3 Me OCH2 -0 3-F-phenyl Isomer 1: 111-112 Isomer 2: Oil 4.134 CH OCH3 Me OCH2 -0 3-C1-phenyl isomer 1: oil isomer 2: oil 4.135 CH OCH3 Me OCHz -0 3-bromo-phenyl isomer 1: resin isomer 2: Harz 4.136 Ν OCH3 Me 0CH2 -0 allyl 4.137 Ν OCH3 Me OCHz -0 3-CF3 -phenyl ** 4.138 Ν OCH3 Me OCHz -0 3-CF3 -phenyl *** 4.139 Ν OCH3 Me-1 2-CF3 Oil 4.140 Ν OCH3 Me-1 2-CH3 Isomer 1: 105-107 Isomer 2: Resin 4.141 Ν NHCH3 Me-1 2-CF3 Resin 4.142 Ν NHCH3 Me-1 2-CH3 Isomer 1: Oil Isomer Structure 2: Youyi 7 6 _ --7 ------ · installed-- (Please read the precautions on the back before filling in This page) C This paper uses Chinese National Standard (CNS) Α4 specifications (210Χ297mm)

、1T 抹 304860 A7 B7 五、發明説明(⑴) 經濟部中央標準局員工消費合作社印製 4.143 CH 0CH3 CN - H 油 4.144 CH 0CH3 CN 0 0 CHs 異構物1 :1 36- 1 38' 異構物2 :樹脂 4.145 CH 0CH3 CN 0 1 4- t- 丁基 油 4.146 CH 0CH3 CN 0 0 苯基 油 4.147 CH 〇CH3 Me 0 0 cf2 CHFz 異構物1:80-82¾ 4.148 CH 0CH3 Me 0 0 CF2 CHClz 4.149 CH 0CH3 Me 0 0 CFz CHBr2 4.150 CH 0CH3 Me 0 0 CF2 CHFCF3 4.151 CH 0CH3 NN 0 0 CFZ CHFz 4.152 CH 0CH3 Me 0 0 cf2 CHFCF3 4.153 N NHCH3 Me 0 0 CFz CHFz 4.154 N NHCH3 Me 0 0 cf2 CHFCF3 4.155 CH 0CH3 Me - 1 4-乙 基 異構物1 :油 異構物2 :油 4.156 CH 0CH3 Me - 1 4- t- 丁基 異構物1 :樹脂 異構物2 :油 4.157 CH 0CH3 Me - 1 4-CF3 異構物1 :樹脂 異構物2 :101-102 4.158 CH 0CH3 Me 0CH2 -1 4-C1 -苯基 4.159 CH ONe CN 0 0 苯基 4.160 N OCH3 Me -S〇2 -0 Et 泡沫 4.161 N NHCH3 Me -S〇z 0 Et 141-143¾ -77- c (請先閲讀背面之注意事項再填寫本頁) 2 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ^^^1 n^i nn ml \ , 1^1 · ^¾. 、ve 線 A7 B7 五、發明説明(I 4 · 162 CH 0CH3 4· 163 CH OCH3 4*164 CH OCHs 4·165 CH OCH3 4.166 CH OCH3 4 . 167 CH OCH3 4· 168 CH OCH3 4.169 CH OCH3 4 · 170 CH OCH3 經濟部中央標準局貝工消費合作社印裝, 1T wipe 304860 A7 B7 V. Description of invention (1) Printed by 4.43 CH 0CH3 CN -H oil 4.144 CH 0CH3 CN 0 0 CHs isomers 1: 1 36- 1 38 'isomers Compound 2: Resin 4.145 CH 0CH3 CN 0 1 4- t-butyl oil 4.146 CH 0CH3 CN 0 0 Phenyl oil 4.147 CH 〇CH3 Me 0 0 cf2 CHFz Isomer 1: 80-82¾ 4.148 CH 0CH3 Me 0 0 CF2 CHClz 4.149 CH 0CH3 Me 0 0 CFz CHBr2 4.150 CH 0CH3 Me 0 0 CF2 CHFCF3 4.151 CH 0CH3 NN 0 0 CFZ CHFz 4.152 CH 0CH3 Me 0 0 cf2 CHFCF3 4.153 N NHCH3 Me 0 0 CFz CHFz 4.154 N NHCH3 Me 0 0 cf2 CHFCF3 4.155 CH 0CH3 Me-1 4-ethyl isomer 1: oil isomer 2: oil 4.156 CH 0CH3 Me-1 4- t-butyl isomer 1: resin isomer 2: oil 4.157 CH 0CH3 Me- 1 4-CF3 isomer 1: Resin isomer 2: 101-102 4.158 CH 0CH3 Me 0CH2 -1 4-C1 -phenyl 4.159 CH ONe CN 0 0 phenyl 4.160 N OCH3 Me -S〇2 -0 Et Foam 4.161 N NHCH3 Me -S〇z 0 Et 141-143¾ -77- c (please read the back Please fill in this page if you need to.) 2 The paper size applies to the Chinese National Standard (CNS) A4 (210X297 mm) ^^^ 1 n ^ i nn ml \, 1 ^ 1 · ^ ¾. Ve line A7 B7 5. Description of the invention (I 4 · 162 CH 0CH3 4 · 163 CH OCH3 4 * 164 CH OCHs 4 · 165 CH OCH3 4.166 CH OCH3 4. 167 CH OCH3 4 · 168 CH OCH3 4.169 CH OCH3 4 · 170 CH OCH3 Ministry of Economic Affairs Central Standards Bureau Printed by Beigong Consumer Cooperative

Me OCH2 - 0 SiNe3 異構物1: 樹脂 異構物2: 油 Me 〇 0 CF2 CHFC1 異構物1: 75- 7 6 ¾ Me 0 0 CF2 CHFBr 異構物1: 樹脂 Me 0 0 CFz CHFCFs 異構物1: 82-84 t: Me S 0 Et 異構物1: 油 異構物2: 油 Me S 0 n- C3 H 7 異構物1: 油 異構物2: 油 Me SCH2 -° 3 3 - C F3 -苯基 Me S〇2 CHz 0 3-CFa -苯基 B D Me SO2 CH2 1 3 - C F2 -苯基 3-FI 1異構物1 :112-11 «異構物2 :榭脂 .”代表化合物沒有取代基—z —B〇 :R 1 / R 2 或 R 3的 . P .或 1 H HHR是 C Η I 3 ,與表標題結構式相符。 **·&gt;Ζ傈使結構#架位於结構元素左邊,而取代基B位於右 邊。例如,化合物4.107之取代基Z—B為一CH2 Ο —苯基。 78 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) (請先聞讀背面之注意事項再填寫本頁) 裝.Me OCH2-0 SiNe3 Isomer 1: Resin Isomer 2: Oil Me 〇0 CF2 CHFC1 Isomer 1: 75- 7 6 ¾ Me 0 0 CF2 CHFBr Isomer 1: Resin Me 0 0 CFz CHFCFs Isomer Compound 1: 82-84 t: Me S 0 Et Isomer 1: Oil Isomer 2: Oil Me S 0 n- C3 H 7 Isomer 1: Oil Isomer 2: Oil Me SCH2-° 3 3 -C F3 -Phenyl Me S〇2 CHz 0 3-CFa -Phenyl BD Me SO2 CH2 1 3-C F2 -Phenyl 3-FI 1 Isomer 1: 112-11 . ”Represents that the compound has no substituent—z—B〇: R 1 / R 2 or R 3. P. Or 1 H HHR is C Η I 3, which is consistent with the table title structure. ** · &gt; Z 傈 使The structure # frame is located on the left of the structural element, and the substituent B is located on the right. For example, the substituent Z-B of compound 4.107 is a CH2 Ο-phenyl. ) (Please read the precautions on the back before filling out this page).

V γ -線 304860 五、發明説明( 表5 A7 B7 〇V γ -line 304860 V. Description of invention (Table 5 A7 B7 〇

Η R7 Η Ή --:-----叫 -裝-- (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 實例 X Υ A R 1 Rs Re R7 P 編號 5.1 CH 0CH3 NMe Me Me Cl Cl 1 5.2 CH 0CH3 NMe H He Cl Cl 1 5 . 3 CH 0CH3 NMe Me Me F F 1 5.4 CH OCH3 NHe Ke Et F F 1 5.5 CH OCH3 NMe Me Me Br Br 1 5.6 CH OCH3 NPh Me Me Cl Cl 1 5.7 CH OCH3 NPh H Me Cl Cl 1 5.8 CH OCH3 NPh Me Et Cl Cl 1 5.9 CH OCH3 0 Me Me Cl Cl 1 5.10 CH OCH3 0 H Me Cl Cl 1 異構物1:86-異構物2:樹脂 異構物3 :樹师I 79- 訂Η R7 Η Ή-: ----- called-installed-- (please read the precautions on the back before filling in this page) Printed example X Υ AR 1 Rs Re R7 P number printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5.1 CH 0CH3 NMe Me Me Cl Cl 1 5.2 CH 0CH3 NMe H He Cl Cl 1 5. 3 CH 0CH3 NMe Me Me FF 1 5.4 CH OCH3 NHe Ke Et FF 1 5.5 CH OCH3 NMe Me Me Br Br 1 5.6 CH OCH3 NPh Me Me Cl Cl 1 5.7 CH OCH3 NPh H Me Cl Cl 1 5.8 CH OCH3 NPh Me Et Cl Cl 1 5.9 CH OCH3 0 Me Me Cl Cl 1 5.10 CH OCH3 0 H Me Cl Cl 1 Isomer 1: 86-isomer 2: Resin isomer 3: Shushu I 79- set

V 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) 五、發明説明(#) A7 B7 經濟部中央標準局員工消費合作社印製 5.11 CH 0CH3 0 Me Me F F 1 5.12 CH 0CH3 0 H Me F F 1 5.13 CH OCH3 0 Me H F F 1 5.14 CH OCH3 0 Me C3 H7 Cl Cl 1 5.15 CH 0CH3 0 Me △ Cl Cl 1 5.16 CH 0CH3 0 △ Me Cl Cl 1 5.17 CH OCH3 0 Me Δ Cl Cl 1 5.18 CH OCH3 0 Me Me Br Br 1 5.19 CH OCH3 0 H Me Br Br 1 5.20 CH OCH3 0 Me Me Cl Cl 2 5.21 CH OCH3 0 H He Cl Cl 2 5.22 CH OCH3 0 Me Me F F 2 5.23 N OCH3 NMe Me Me Cl Cl 1 5.24 N OCH3 NNe H Me Cl Cl 1 5.25 N OCH3 NHe Me He F F 1 5.26 N OCH3 NMe Me Et F F 1 5.27 N OCH3 NHe Me Br Br 1 5.28 N OCH3 NPh He Me Cl Cl 1 5.29 N OCH3 NPh H Me Cl Cl 1 5.30 N OCH3 NPh Me Et Cl Cl 1 5.31 N OCH3 0 Me Me Cl Cl 1 5.32 N OCH3 0 H Me Cl Cl 1 5.33 N OCH3 0 Me Me F F 1 -80- ^ ·裝 訂 ( 故 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(2丨Ο X 297公釐) 五、發明説明(卩0 A7 B7 經濟部中央標準局員工消費合作社印製 5.34 Ν OCH3 0 H Me F F 1 5.35 Ν 0CH3 0 He H F F 1 5.36 Ν OCH3 0 Me c3 H7 Cl Cl 1 5.37 Ν OCH3 0 Me Δ Cl Cl 1 5.38 Ν 0CH3 0 Δ Me Cl Cl 1 5.39 Ν OCH3 0 Me △ Cl Cl 1 5.40 Ν OCH3 0 Me Me Br Br 1 5.41 Ν OCH3 0 H Me Br Br 1 5.42 Ν OCH3 0 Me Me Cl Cl 2 5.43 Ν OCH3 0 H Me Cl Cl 2 5.44 Ν OCH3 0 Me Me F F 2 5.45 Ν NHCH3 NMe Me Me Cl Cl 1 5.46 Ν NHCH3 NNe H Me Cl Cl 1 5.47 Ν NHCH3 NMe Me Me F F 1 5.48 Ν NHCH3 NMe Me Et F F 1 5.49 Ν HHCH3 NMe Me Br Br 1 5.50 CH OCHs 0 Me Me H H 1 異構物1:油 異構物2:油 5.51 Ν OCH3 0 Me Me Cl Cl 1 異構物1:油 5.52 Ν NHCH3 0 Me Me Cl Cl 1 137-139^ 5.53 Ν HHCH3 0 Me Me Cl Cl 1 5.54 Ν NHCH3 0 H Me Cl Cl 1 5.55 Ν NHCH3 0 Me Me F F 1 -81- --------------^ —裝------訂-----^ -線 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 五、發明説明(#) A7 B7 5.56 N NHCH3 0 Η Me F F 1 5.57 N NHCH3 0 Me K F F 1 5.58 N NHCH3 0 Me Me Cl Cl 2 5.59 N KHCH3 0 Η Me Cl Cl 2 5.60 N NHCHa 0 Me Me F F 2 以及化合物 61V This paper scale is applicable to the Chinese National Standard (CNS) Α4 specification (210X297 mm) V. Invention description (#) A7 B7 Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5.11 CH 0CH3 0 Me Me FF 1 5.12 CH 0CH3 0 H Me FF 1 5.13 CH OCH3 0 Me HFF 1 5.14 CH OCH3 0 Me C3 H7 Cl Cl 1 5.15 CH 0CH3 0 Me △ Cl Cl 1 5.16 CH 0CH3 0 △ Me Cl Cl 1 5.17 CH OCH3 0 Me Δ Cl Cl 1 5.18 CH OCH3 0 Me Me Br Br 1 5.19 CH OCH3 0 H Me Br Br 1 5.20 CH OCH3 0 Me Me Cl Cl 2 5.21 CH OCH3 0 H He Cl Cl 2 5.22 CH OCH3 0 Me Me FF 2 5.23 N OCH3 NMe Me Me Cl Cl 1 5.24 N OCH3 NNe H Me Cl Cl 1 5.25 N OCH3 NHe Me He FF 1 5.26 N OCH3 NMe Me Et FF 1 5.27 N OCH3 NHe Me Br Br 1 5.28 N OCH3 NPh He Me Cl Cl 1 5.29 N OCH3 NPh H Me Cl Cl 1 5.30 N OCH3 NPh Me Et Cl Cl 1 5.31 N OCH3 0 Me Me Cl Cl 1 5.32 N OCH3 0 H Me Cl Cl 1 5.33 N OCH3 0 Me Me FF 1 -80- ^ Binding (Therefore (please read the back of the first (Notes and then fill out this page) This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (2 丨 Ο X 297mm) V. Explain clearly (ie 0 A7 B7 Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy 5.34 Ν OCH3 0 H Me FF 1 5.35 Ν 0CH3 0 He HFF 1 5.36 Ν OCH3 0 Me c3 H7 Cl Cl 1 5.37 Ν OCH3 0 Me Δ Cl Cl 1 5.38 Ν 0CH3 0 Δ Me Cl Cl 1 5.39 Ν OCH3 0 Me △ Cl Cl 1 5.40 Ν OCH3 0 Me Me Br Br 1 5.41 Ν OCH3 0 H Me Br Br 1 5.42 Ν OCH3 0 Me Me Cl Cl 2 5.43 Ν OCH3 0 H Me Cl Cl 2 5.44 Ν OCH3 0 Me Me FF 2 5.45 Ν NHCH3 NMe Me Me Cl Cl 1 5.46 Ν NHCH3 NNe H Me Cl Cl 1 5.47 Ν NHCH3 NMe Me Me FF 1 5.48 Ν NHCH3 NMe Me Et FF 1 5.49 Ν HHCH3 NMe Me Br Br 1 5.50 CH OCHs 0 Me Me HH 1 Isomer 1: Oil Isomer 2: Oil 5.51 Ν OCH3 0 Me Me Cl Cl 1 Isomer 1: Oil 5.52 Ν NHCH3 0 Me Me Cl Cl 1 137 -139 ^ 5.53 Ν HHCH3 0 Me Me Cl Cl 1 5.54 Ν NHCH3 0 H Me Cl Cl 1 5.55 Ν NHCH3 0 Me Me FF 1 -81- -------------- ^ -installed- ----- Subscribe ----- ^ -Line (please read the precautions on the back before filling in this page) This paper size is applicable to China National Standard (CNS) Α4 specification (210Χ297mm) Description of the invention (#) A7 B7 5.56 N NHCH3 0 Η Me FF 1 5.57 N NHCH3 0 Me KFF 1 5.58 N NHCH3 0 Me Me Cl Cl 2 5.59 N KHCH3 0 Η Me Cl Cl 2 5.60 N NHCHa 0 Me Me FF 2 and Compound 61

異構物1: 113-1151C /異構物2:油 (請先閱讀背面之注意事項再填寫本頁) —-------^ I 裝------訂-----『' ..it 經濟部中央標準局員工消費合作社印製 〇 6 2 h3cIsomer 1: 113-1151C / Isomer 2: Oil (please read the precautions on the back before filling this page) —------- ^ I 装 ------ 定 ---- -『'..It Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 〇6 2 h3c

外 Z、CH3Outer Z, CH3

異構物1:油/異構物2:油 82 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 304860 A7 B7 五、發明説明(Μ ) 經濟部中央標準局員工消費合作社印製 〇Isomer 1: Oil / Isomer 2: Oil 82 This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 304860 A7 B7 V. Description of Invention (Μ) Printed by the Employees Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs System

1 55 - 1 6 0 t: (請先閱讀背面之注意事項再填寫本頁)1 55-1 6 0 t: (Please read the notes on the back before filling this page)

^^^1 —^1 ^^^1 n .^ϋ I - - I I m 1^1 In - m I nn s I - 、一(aJ- ^1.^1 1—ii (. I 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 五、發明説明(β) .65 5.66 A7 B7^^^ 1 — ^ 1 ^^^ 1 n. ^ Ϋ I--II m 1 ^ 1 In-m I nn s I-、 一 (aJ- ^ 1. ^ 1 1—ii (. I This paper size Applicable to China National Standard (CNS) A4 specification (210X 297mm) V. Description of invention (β) .65 5.66 A7 B7

〇 H3C〇 H3C

Br 異構物1:109-1101/異構物2:樹脂Br Isomer 1: 109-1101 / Isomer 2: Resin

(請先閲讀背面之注意事項再填寫本頁)(Please read the notes on the back before filling this page)

^^1 —ii ^^1 I 8- I I - - I— --- I m. I— ^ - ...... I - - - - -- ml - .n in - —...... —' I 經濟部中央標準局員工消費合作社印製 異構物1:113-13310/異構物2:樹脚^^ 1 —ii ^^ 1 I 8- II--I— --- I m. I— ^-...... I-----ml-.n in-—... .. — 'I Printed Isomers 1: 13-13310 / Isomer 2: Tree Feet by the Employees ’Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

**物理資料:Ri / Rz或R3的ι.Ρ.或1 H NMR -84- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7 B7 五、發明説明(Μ ) 表6** Physical data: ι.Ρ. of Ri / Rz or R3 or 1 H NMR -84- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) A7 B7 V. Invention description (Μ) Table 6

(請先閱讀背面之注意事項再填寫本頁) -裝. 經濟部中央標準局員工消費合作社印製 實例 X Y Ri ΤΛ n B或D 物理資料 编號 6.1 CH 0CH3 He 0 0 烯丙基 油 6 . 2 CH 0CH3 Me 1 4-溴 異構物1:油 異構物2:油 6.3 N 0CH3 Me 0 0 烯基 油 6.4 N 0CH3 Me - 1 4-溴 131-1321 6.5 N NHCH3 He 0 - 烯基 油 6.6 N NHCH3 Me - 1 4-溴 異構物1 ·. 11 7 - 1 異構物2:油 6.7 CH 0CH3 Me - 1 4-甲基- 異構物1 : 2 . 10 異構物2:2 . 08 6.8 N OCH3 He - 1 4-甲基- 6 . 9 N NHCH3 Me 1 4_甲基- -85- 、va 線 本紙張尺度適用中國國家標隼(CNS ) A4規格(210X 297公釐) 五、發明説明(v A7 B7(Please read the precautions on the back before filling out this page)-Pack. Printed example of XY Ri ΤΛ n B or D printed by the Employees ’Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Physical data number 6.1 CH 0CH3 He 0 0 Allyl oil 6. 2 CH 0CH3 Me 1 4-bromo isomer 1: oil isomer 2: oil 6.3 N 0CH3 Me 0 0 alkenyl oil 6.4 N 0CH3 Me-1 4-bromo 131-1321 6.5 N NHCH3 He 0-alkenyl oil 6.6 N NHCH3 Me-1 4-bromo isomer 1 ·. 11 7-1 isomer 2: oil 6.7 CH 0CH3 Me-1 4-methyl- isomer 1: 2. 10 isomer 2: 2 . 08 6.8 N OCH3 He-1 4-methyl- 6. 9 N NHCH3 Me 1 4_methyl- -85-, va line paper size is applicable to China National Standard Falcon (CNS) A4 specification (210X 297 mm) 5. Description of the invention (v A7 B7

〇 H3C〇 H3C

A 'r3 ^ ·裝 ,言 ( 泳 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印裝 -8 6 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7 B7 五、發明説明(幻 經濟部中央標準局員工消費合作社印製 |例 Y A R i Rz R3 1號 或 NR3 R 1 OEt NMe Me Me Me 2 OEt NHe H Me 6-CF3 -2 3 OEt NMe Me Δ 6-CFs -2 4 OEt NMe Me H 苯基 5 OEt NMe Me Me 苯基 6 OEt NMe Δ Me 苯基 7 OEt NMe H Me 4-瞟啉基 8 OEt NPh H Me 苯基 9 OEt NPh Me Me 苯基 10 OEt NPh Me Δ 苯基 11 OEt NPh △ Me 苯基 12 OEt 0 Me Me Me 13 OEt 0 H Me Me 14 OEt 0 Δ Me Me -87- 物理資料** (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 五、發明説明(8二) A7 B7 經濟部中央樣準局員工消費合作社印製 7.15 OEt 0 Me Δ Ne 7.16 OEt 0 Me H Ne 7.17 OEt 0 Me Me 苯基 7.18 OEt 0 Me Me 苄基 7.19 OEt 0 Me Me 3-CF3 -2-¾ 啶基 7.20 OEt 0 Me Me 3-CF2 -苯基 7.21 NHZ NMe Me Δ 3-CF3 -苯基 7.22 NHZ NMe H Me 4-CF3 -苯基 7.23 NHz NMe Me Me 4-CF3 -苯基 7.24 HHZ NMe Me He 2-氱苯基 7.25 NHz NMe Me Me 3-氨苯基 7.26 nh2 NMe Me Me 4-氰苯基 7.27 nh2 0 Me Me 苯基 7.28 nh2 0 Me Me Ne 7.29 NHz 0 Me Me 苄基 7.30 NHz 0 Me Me Et 7.31 NHz 0 H Me Et 7.32 NHz 0 △ Ne Et 7.33 nh2 0 Me Δ Et 7.34 NHz 0 Me H Et 7.35 NHz 0 Me Me 甲氣基甲基 7.36 NHZ 0 Me △ 甲氣基甲基 7.37 nh2 0 △ Ne 甲氣基甲基 -88- —;------1 -裝------訂-----線 (請先聞讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4g ( 210X297公釐) 304860 五、發明説明(8)) A7 B7 經濟部中央標準局員工消費合作社印製 7.38 KHz 0 Me Me 乙氣基甲基 7.39 nh2 0 H Me 丙烯基 7.40 NHz 0 Me Me 氣甲基 7.41 NHz 0 Me Me Η 7.42 NHz 0 Me Me CF3 CHz 7.43 nh2 0 Δ Me cf3 ch2 7.44 NH2 0 Me H CF3 CHz 7.45 NHz 0 Me H CF3 CHz CHz 7.46 nh2 0 Me Me CF3 CHz ch2 7.47 NHz 0 Me Me CF3 CHz ch2 CHz 7.48 NHz 0 Δ Me cf3 ch2 ch2 ch2 7.49 NHEt NMe Me Δ 3-CF3 -苯基 7.50 NHEt NNe H Me 4-CF3 -苯基 7.51 NHEt NMe Me Me 4-C F 3 -苯基 7.52 NHEt NMe He Me 2-氯苯基 7.53 NHEt NHe Me He 3-氨苯基 7.54 NHEt NHe Me He 4-氮苯基 7.55 HHEt 0 Me Me 苯基 7.56 NHEt 0 Me Me Me 7.57 NHEt 0 Me Me 苄基 7.58 NHEt 0 Me Me Et 7.59 HHEt 0 H Me Et 7.60 NHEt 0 Δ Me Et 一 89- (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4g ( 210X297公釐) 五、發明説明(艸) A7 B7 經濟部中央標隼局員工消費合作社印製 7.61 NHEt 0 Me △ Et 7.62 NHEt 0 Me H Et 7.63 NHEt 0 Me Me 甲氣基甲基 7.64 NHEt 0 Me Δ 甲氣基甲基 7.65 NHEt 0 △ Ne 甲氣基甲基 7.66 NHEt 0 Me Me 乙氣基甲基 7.67 NHEt 0 H Me 丙烯基 7.68 NHEt 0 Me Me 氱甲基 7.69 NHEt 0 Me Me Η 7.70 NHEt 0 Me Me CF3 CH2 7.71 NHEt 0 Δ Me CF3 CHz 7.72 NHEt 0 Me H cf3 ch2 7.73 NHEt 0 Me H CF3 CHz CH2 7 .74 NHEt 0 Me Ne CF3 CHz CH2 7.75 NHEt 0 Me Me cf3 ch2 ch2 CHZ 7.76 NHEt 0 △ Me CF3 CHz CH2 ch2 7.77 N(Me)2 NMe Me △ 3-CF3 -苯基 7.78 H(Me)z NNe H Me 4-CF3 -苯基 7.79 N(Me)2 NMe Me Ne 4-CF3 -苯基 7.80 N(Me)z NHe Me Me 2-氰苯基 7.81 H(Me)2 NHe Me Me 3-氨苯基 7.82 N(Me)z NHe Me Me 4-氯苯基 7.83 M(Me)z 0 Me Me 苯基 -90- —· 裝 訂 叫 —線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) S0486Q, 五、發明説明(胗) 經濟部中央標準局員工消費合作社印製 7.84 H(Me)z 0 Me Me Me 7.85 Η(Μβ)2 0 Me Me 苄基 7.86 Ν(Μβ)2 0 Me Me Et 7.87 H(Me)2 0 H Me Et 7.88 N(Me)2 0 △ Me Et 7.89 H(Me)2 0 He △ Et 7.90 N(Me)2 0 Me H Et 7.91 M(Me)z 0 Me Me 甲氣基甲基 7.92 N(Me)2 0 He Δ 甲氣基甲基 7.93 N(Me)z 0 △ Me 甲«基甲基 7.94 N(Me)z 0 Me Me 乙氣基甲基 7 . 95 M(Me)2 0 H Me 丙烯基 7.96 M(Me)z 0 Me He 氯甲基 7.97 N(Me)z 0 Me Me Η 7.98 N(Me)2 0 Me Me CF3 CHz 7.99 N(Me)2 0 △ Me CF3 CHz 7.100 N(Me)z 0 Me H CF3 CHz 7.101 H(Me)z 0 Me H CF3 CHz CHz 7.102 N(Me)z 0 Me Me CF3 CHz ch2 7.103 H(Me)2 0 Me Me CF3 CHz CH2 ch2 7.104 N(Me)z 0 △ Me CF3 CHz CHz CHz ^ 裝 i ( ^ (請先閲讀背面之注意事項再填寫本頁) -91-本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) A7 B7 ®〇486〇 五、發明説明(0 ) 2.式I活性成份之配方資例(%為重量百分比) 資例2. 1:可濕潤粉未 a) b) c) 表1-7活性成份 25X 50Z 75* 木質素磺酸納 5X 5X - 月桂基硫酸納 3% - 5X 二異丁基莱磺酸納 - 6X 102 辛基酚聚乙二酵醚(7-8·ο1 Ε0) - 2% - 高分散二氣化矽 52 10X 10% 高嶺土 62% 27X - (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 活性成份輿添加劃徹底混合,混合物被擻底的在一合 適的研磨機中研磨,得到可濕濶的粉未,可被水稀》成任 何濃度的懸浮液。 實例2 . 2乳化液灞縮液 表1-7活性成份 10Χ 辛基酚聚乙二醇_ (4-5·ο1 Ε0) 3* 十二基苯磺酸鈣 3Ϊ 琢己酮 34Χ 二甲苯混合物 50ί 任何希望酿度的乳化液可從任何此種濃度加水稀釋加 以製備。 實例2.3 :粉應 a) b) 表1-7活性成份 5% sx 滑石 95% - -92- 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公嫠} 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(Μ ) 高嶺土 - 92J; 活性成份與載鼸混合•混合物在一合適的研磨機中研 磨,得到可立®可供使用的粉塵。 實例2.4 :擠出物顙粒 表1-7活性成份 102 木霣素磺酸納 2% 羧酸甲基纖維素 IX 髙嶺土 87* 活性成份與添加劑混合,混合物被研磨,並用水灞濶 之,混合物被擠出, 接箸於一空氣蒸氣中乾燥。 實例2.5塗佈顆粒 表1-7活性成份 3Z 聚乙二酵(HW 2 0 0) 3X 离嶺土 94X (MW為分子量) 顆粒撤细的活性成份在混合器中被均勻的塗佈於已經 被聚乙二酵漉箱的离嶺土,以此方法得到無襄塗佈顆粒。 實例2.6:懸浮液濃缩物 表1-7之活性成份 40客 乙二酵 m 壬基酚聚乙二酵醚(15·〇1 EO) SX 木質素磺酸納 10*A 'r3 ^ · Install, say (swim (please read the precautions on the back before filling out this page) Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs-8 6 This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 Mm) A7 B7 V. Description of invention (printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs | Example YAR i Rz R3 No. 1 or NR3 R 1 OEt NMe Me Me Me 2 OEt NHe H Me 6-CF3 -2 3 OEt NMe Me Δ 6-CFs -2 4 OEt NMe Me H phenyl 5 OEt NMe Me Me phenyl 6 OEt NMe Δ Me phenyl 7 OEt NMe H Me 4-oxolinyl 8 OEt NPh H Me phenyl 9 OEt NPh Me Me Phenyl 10 OEt NPh Me Δ Phenyl 11 OEt NPh △ Me Phenyl 12 OEt 0 Me Me Me 13 OEt 0 H Me Me 14 OEt 0 Δ Me Me -87- Physical Information ** (Please read the notes on the back first (Fill in this page again) This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 5. Description of the invention (8 2) A7 B7 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy 7.15 OEt 0 Me Δ Ne 7.16 OEt 0 Me H Ne 7.17 OEt 0 Me Me Phenyl 7.18 OEt 0 Me Me Benzyl 7.19 OEt 0 Me Me 3-CF3 -2-¾ pyridyl 7.20 OEt 0 Me Me 3-CF2 -phenyl 7.21 NHZ NMe Me Δ 3-CF3 -phenyl 7.22 NHZ NMe H Me 4-CF3 -phenyl 7.23 NHz NMe Me Me 4-CF3 -Phenyl 7.24 HHZ NMe Me He 2-triphenyl 7.25 NHz NMe Me Me 3-aminophenyl 7.26 nh2 NMe Me Me 4-cyanophenyl 7.27 nh2 0 Me Me phenyl 7.28 nh2 0 Me Me Ne 7.29 NHz 0 Me Me Benzyl 7.30 NHz 0 Me Me Et 7.31 NHz 0 H Me Et 7.32 NHz 0 △ Ne Et 7.33 nh2 0 Me Δ Et 7.34 NHz 0 Me H Et 7.35 NHz 0 Me Me Methoxymethyl 7.36 NHZ 0 Me △ Methane Methyl 7.37 nh2 0 △ Ne Methoxymethyl-88--; ------ 1 -installed ------ ordered-line (please read the precautions on the back first (Fill in this page) This paper scale is applicable to the Chinese National Standard (CNS) A4g (210X297mm) 304860 V. Description of the invention (8)) A7 B7 Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economics 7.38 KHz 0 Me Me Base 7.39 nh2 0 H Me propenyl 7.40 NHz 0 Me Me gas methyl 7.41 NHz 0 Me Me Η 7.42 NHz 0 Me Me CF3 CHz 7.43 nh2 0 Δ Me cf3 ch2 7.44 NH2 0 Me H CF3 CHz 7.45 NHz 0 Me H CF3 CHz CHz 7.46 nh2 0 Me Me CF3 CHz ch2 7.47 NHz 0 Me Me CF3 CHz ch2 CHz 7.48 NHz 0 Δ Me cf3 ch2 ch2 ch2 7.49 NHEt NMe Me Δ 3-CF3 -phenyl 7.50 NHEt NNe H Me 4-CF3 -phenyl 7.51 NHEt NMe Me Me 4-CF 3 -phenyl 7.52 NHEt NMe He Me 2-chlorophenyl 7.53 NHEt NHe Me He 3-aminophenyl 7.54 NHEt NHe Me He 4-nitrophenyl 7.55 HHEt 0 Me Me phenyl 7.56 NHEt 0 Me Me Me 7.57 NHEt 0 Me Me benzyl 7.58 NHEt 0 Me Me Et 7.59 HHEt 0 H Me Et 7.60 NHEt 0 Δ Me Et-89- (please read the precautions on the back before filling this page) This paper size is applicable China National Standards (CNS) A4g (210X297mm) V. Description of invention (pocket) A7 B7 Printed by the Ministry of Economy Central Standard Falcon Bureau Employee Consumer Cooperative 7.61 NHEt 0 Me △ Et 7.62 NHEt 0 Me H Et 7.63 NHEt 0 Me Me A Aminomethyl 7.64 NHEt 0 Me Δ Methylmethyl 7.65 NHEt 0 △ Ne Methylmethyl 7.66 NHEt 0 Me Me Ethylmethyl 7.67 NHEt 0 H Me Propylene 7.68 NHEt 0 Me Me 氱 methyl 7.69 NHEt 0 Me Me Η 7.70 NHEt 0 Me Me CF3 CH2 7.71 NHE t 0 Δ Me CF3 CHz 7.72 NHEt 0 Me H cf3 ch2 7.73 NHEt 0 Me H CF3 CHz CH2 7.74 NHEt 0 Me Ne CF3 CHz CH2 7.75 NHEt 0 Me Me cf3 ch2 ch2 CHZ 7.76 NHEt 0 △ Me CF3 CHz CH2 ch2 7.77 N (Me) 2 NMe Me △ 3-CF3 -phenyl 7.78 H (Me) z NNe H Me 4-CF3 -phenyl 7.79 N (Me) 2 NMe Me Ne 4-CF3 -phenyl 7.80 N (Me) z NHe Me Me 2-cyanophenyl 7.81 H (Me) 2 NHe Me Me 3-aminophenyl 7.82 N (Me) z NHe Me Me 4-chlorophenyl 7.83 M (Me) z 0 Me Me Phenyl-90- — · Binding call-line (please read the precautions on the back before filling in this page) This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) S0486Q, V. Description of invention (girdle) Central Ministry of Economic Affairs 7.84 H (Me) z 0 Me Me Me 7.85 Η (Μβ) 2 0 Me Me benzyl 7.86 Ν (Μβ) 2 0 Me Me Et 7.87 H (Me) 2 0 H Me Et 7.88 N (Me) 2 0 △ Me Et 7.89 H (Me) 2 0 He △ Et 7.90 N (Me) 2 0 Me H Et 7.91 M (Me) z 0 Me Me Methoxymethyl 7.92 N (Me) 2 0 He Δ Methoxymethyl 7.93 N (Me) z 0 △ Me Methoxymethyl 7.94 N (Me) z 0 Me Me Ethoxymethyl 7.95 M (Me) 2 0 H Me Propylene 7.96 M (Me) z 0 Me He Chloromethyl 7.97 N (Me) z 0 Me Me Η 7.98 N (Me) 2 0 Me Me CF3 CHz 7.99 N (Me) 2 0 △ Me CF3 CHz 7.100 N (Me) z 0 Me H CF3 CHz 7.101 H (Me) z 0 Me H CF3 CHz CHz 7.102 N (Me) z 0 Me Me CF3 CHz ch2 7.103 H (Me) 2 0 Me Me CF3 CHz CH2 ch2 7.104 N (Me) z 0 △ Me CF3 CHz CHz CHz ^ Pack i (^ (Please read the precautions on the back before filling this page) -91-This paper size is applicable China National Standards (CNS) A4 specification (210X297mm) A7 B7 ® 〇486〇 V. Description of invention (0) 2. Formula I of active ingredient formula (% is weight percentage) Case 2: 1: Wettable Powder a) b) c) Table 1-7 Active ingredients 25X 50Z 75 * Sodium lignosulfonate 5X 5X-Sodium lauryl sulfate 3%-5X Sodium diisobutyl sulfonate-6X 102 Octylphenol polyethylene Diester (7-8 · ο1 Ε0)-2%-High-dispersed Di-Volatilized Silicon 52 10X 10% Kaolin 62% 27X-(Please read the precautions on the back before filling this page) Employee consumption of the Central Standards Bureau of the Ministry of Economic Affairs Cooperatives print active ingredients and add them thoroughly Together, milled in a suitable mill mixture was shake bottom to obtain the wettable powder Kuo, water can be thin "into any concentration suspension. Example 2. 2 Emulsions and condensates Table 1-7 Active ingredient 10Χ Octylphenol polyethylene glycol_ (4-5 · ο1 Ε0) 3 * calcium dodecylbenzenesulfonate 3Ϊ hexanone 34Χ xylene mixture 50ί any The desired degree of emulsion can be prepared from any such concentration diluted with water. Example 2.3: Powder should be a) b) Table 1-7 Active ingredient 5% sx talc 95%--92- This paper scale is applicable to China National Standard (CNS) Α4 specification (210X297 public daughter) Employee Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs Printed A7 B7 V. Description of the invention (Μ) Kaolin-92J; the active ingredient is mixed with the loaded mule • The mixture is ground in a suitable grinder to obtain the available dust of Keli®. Example 2.4: Extrudate pellet Table 1-7 Active Ingredients 102 Sodium Canthylsulfonate 2% Methyl Cellulose Carboxylic Acid IX Naolin 87 * The active ingredients are mixed with additives, the mixture is ground, and the mixture is extruded with water It is dried in an air vapor. Example 2.5 Coated particles Table 1-7 Active ingredients 3Z Polyoxinase (HW 2 0 0) 3X Chilling clay 94X (MW is the molecular weight) The active ingredients of fine particles are removed in the mixer Apply evenly to the kaolin that has been packed with glyphosate to obtain Wuxiang coated particles in this way. Example 2.6: Suspension Concentrate The active ingredients in Table 1-7 are 40 g Polyphenol Glyoxylate (15 · 〇1 EO) SX Sodium Lignosulfonate 10 *

羧酸甲基鐵維素 U -93- 本紙張尺度適用中國國家梯準(CNS ) A4規格(210X297公釐) 7 ^ .裝 i ( 咏 (請先閱讀背面之注意事項再填寫本頁) 3〇486〇 五、發明説明U” A7 B7 37J:甲醛水溶液 0 . 2X 75ί水性乳液的矽酮油 0.8Z 水 32X 顆粒 微细 的 活 性 成 份與 添加劑徹底混合 •得 到一 種驗 浮液 .可 被水 稀 釋 成 任 何濃 度的懲浮液。 3 . 生物 性實 例 A ) 微生 物活 性 實例 B — 1 : 抗 蕃 茄 之 Phyt ophthora infes tans 之作 性 (a )治 療活 性 蕃茄 植物 c V 9» Ro ter Gno·”生長三邇, 然後噗予徽篇 的動 物孢 子« 浮 物 f 在 18 到2 0 1C及銪和 澜濕 大氣 之室 内培 餐。 2 4 小 時 之 後 ,停 止灞氣供窿。植 物乾 枯之 後, (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局貝工消費合作社印製 被喷予包括被譎配成可濕潤粉末之濃度為20 0 p pm之 活性成份混合物。喷灑之塗覆乾燥之後,将植物取回到潮 濕室内置放4天。過了這段時間之後發展出來的葉斑之數 目和大小被用來評估試驗物質的活性。 (b)預防条统性活性 將濃度為60 ppm (相對於土壤讎積)之被調配成 可濕潤粉之活性成份投予鑷内之已生長3邇之蕃茄植物cv. ”Roter Gnoa”。植物靜置3天之後,葉子底面被喷予Carboxymethyl methionine U-93- This paper scale is applicable to China National Standards (CNS) A4 specification (210X297mm) 7 ^. Install i (chant (please read the precautions on the back before filling this page) 3 〇486〇 V. Description of the invention U ”A7 B7 37J: Formaldehyde aqueous solution 0.2X 75ί silicone oil 0.8Z water 32X water 32X particles of finely mixed active ingredients and additives thoroughly • to obtain a float test liquid. Can be diluted into Any concentration of punishment liquid. 3. Biological example A) Example of microbial activity B-1: The anti-tomato phyt ophthora infes tans (a) therapeutically active tomato plant c V 9 »Ro ter Gno Then, the animal spores in the poems of the emblem «Float f are cultivated indoors at 18 to 201 1C and in the atmosphere of Europium and Lanshui. After 2 4 hours, stop supplying the gas. After the plants have dried up (please read the precautions on the back before filling out this page) Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, it is sprayed to include an active ingredient mixture that is formulated into a wettable powder of 20 ppm . After the spray coating has dried, the plants are taken back into the damp chamber and placed for 4 days. The number and size of leaf spots developed after this period of time were used to assess the activity of the test substance. (b) Preventive systemic activity The active ingredient formulated as a wettable powder at a concentration of 60 ppm (relative to soil volume) is administered to the tomato plant cv. "Roter Gnoa" which has been grown for 3 hours in tweezers. After the plant was allowed to stand for 3 days, the bottom of the leaves was sprayed

Phy tophthora inf estans之動物孢子懸浮物。該植物再於 1 8到2 Ot:及飽和潮濕大氣的喷灌室内置放5天。之後 ,發展出典型的葉斑,採用其數目和大小評估試驗物霣的 -94- 本紙張尺度適用中國國家標隼(CNS ) A4規格(210X297公釐) 304860 A7 B7 五、發明説明u?) 活性。 未經處理但受到威染的對照組植物顯示1 〇 〇%之® 染率,使用表中一種式I的活性成份者,特別是使1. 5 • 1. 24, 1. 117, 2. 24, 2. 74 和 3. 2 4之化合物,讓以上兩組試驗的感染率降低到20%或以 下。 實例 B — 2:抗蕕萄之 Plasiopara viticola(Bert. e t C u r t. ) ( B e r 1. e t D e T ο n i)活性 (a )殘留預防活性 «萄小枝cv. &quot;Chassels”在溫室中生長,當長成10 葉階段,對其中3株植物_予混合物(200p pm之活 性成份)。待植物上之嗔塗塗覆物乾燥之後,在藥子底面 均勻地植入徽_孢子懲浮物。接著使植物保持在禳濕室内 逹8天。之後.對照组植物已經淸楚的發展出病症。受處 理植物之受損部份數目和大小被用來評估試驗物質的活性 〇 (b)治療活性 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再填寫本頁) 葡萄小枝CV. ” Chassels”在溫室中生長,當長成10 葉陏段,對其葉子底面喷予Plasiopara viticola之孢子懸 浮物。等植物在潮濕室内置放24小時之後,被噴予活性 成份混合物(200 ppm之活性成份)。接著使植物保 持在潮濕室内達7天。之後,對照组植物已經清楚的發展 出病症。受處理植物之受損部份數目和大小被用來評估試 -95- 本紙張尺度適用中國國家標準(CNS ) Λ4規格(210X297公釐) 經濟部中央標準局員工消費合作社印装 A7 B7__ 五、發明説明(?叫 驗物質的活性。 與對照组植物比較,經過式I活性成份«理之檯物戚 染率為2 0%或以下。 實例 B-3 :對甜菜(B e t a v u 1 g a r i s ) P y t h i u d e b a r y a n u 之活性 徽菌在消毒遘的燕麥上生長,将其加入土«和砂之混 合物中。將此經遇種植之土壤媾入花盆,種植甜菜。種植 之後,馬上將被調配成可灞®粉末之試驗製物以水性》浮 物形式(20p pm活性成份,相對於土孃)被倒入土禳 。将花盆置於20到24Ό溫度中遽2到3邏。其两軽噴 獮水份,使土壤保持均勻潮猫。進行評估畤,算出甜菜植 物出芽數目及健康和受感染植物數目。 (b)種子包敷後之活性 徽_在消毒遇的燕麥上生長,將其加入土壤和砂之混 合物中。將此經遇種植之土壤填入花盆和種植被包敷著經 讕配成包敷種子粉末(lOOOppm活性成份,相_於 種子重量)試驗製備物的甜菜。花盆輿種子被置於20— 24C之溫室達2到3通。輕輕噴爾水份,使土壤保持均 勻潮獯。進行評估時,算出甜菜植物出芽數目及键康和受 威染植物數目。用式I活性成份進行處理,待別是化合物 1. 5, 1. 24, 1. 117, 2. 24, 2. 74 和 3. 24,超遇80%之植物發芽,外觀健康。在對照组 之花盆中,只有少數外觀不健康之植物發芽。 - 9 6 _ 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) I.------------、玎-----^ (請先閲讀背面之注意事項再填寫本頁) A7 B7 304860 五、發明説明(7 / ) 實例B — 4 :對落花生之Cercospora arachidicola之殘留 保護活性 1 0到1 5公分离的落花生被《鼸水性嗔灑混合物( 〇. 02%活性成份)到滴黏,48小時之後,植入徽醣 之頂端芽胞懸浮物。植物在2 1 t:及高度潮灘大氣中培餐 72小時接著置於溫室中,直到出現典型葉子斑點。接種 之後以藥斑數目及大小來評估活性成份的活性。式I活性 成份使葉斑占葉子面積小於1 0%。在某些情況下,此疾 病幾乎完全被消除(0 - 5%威染)。 實例B - 5 :對小麥Puccinia graiinis之活性 a )殘留保護活性 種植6天之後,小麥植物被水性噴鼸涯合物(0. 0 02活性成份)噴漏到滴點,24小時之後,接種徽鐘之 111:0111〇3?(^0懸浮物。培養4 8小時之後(條件為2〇1〇, 相對濕度95到100%),將植物置於22*C之ffl室中 ,接種12天之後評估綉讓疱發展情況。 b )条統活性 種植5天之後,將水性噴灌混合物(0. 006%活 性成份,相銳於土壤龌積)倒入小麥植物四周。小心避免 啧繼混合物與任何地面上的植物接觸。48小時之後,對 植物接種ureidospore徽齠懸浮物。接種之後48小畤後( 條件為20TC,相對濕度為95到100%),將植物置 於2 2它粗室内。接種後12天,評估_釀疱發展情況。 -97- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 丨^------「I裝------訂-----^ 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央樣準局貝工消費合作社印製 經濟部中央梂準局員工消費合作社印製 A7 ___B7__ 五、發明説明) 式I化合物,特別是表1中1. 5, 1.24, 1. 11 7, 2. 74等化合物顯著減少徽趙戚染,在某些情況下 減少到1 0 — 0 %。 實例B — 6 :對稻米Pyricularia oryzae之活性 a )殘留預防活性 稻米植物生長2遇後被水性噴灑鹿合物(0. 02% 活性成份0噴漏到滴點,4 8小時後,接種徽鹧conidi a想 浮物。接種5天後評估徽鯖戚染情況,期間相對瀰度被保 持在95到100%,溫度為22&quot;C。 b )系统活性 對水性嗔灑混合物(0. 006%活性成份,相對於 土壤體稹)倒入生長2遇稻米四周。小心避免噴灑混合物 輿任何地面上的植物接觸。然後將花盆装入數量使稻米最 低之莖部位浸入其中的水。9 6小時之後,對植物接種 conidi a徽菌懸浮物,並保持在相對濕度為9 5到100% 及溫度為241C條件下。在多種情況下,式I化合物預防 受威染植物病況惡化。 實例B-7 :對蘋果Venturia inaequalis之殘留保謹活性 含10到20公分新鮮嫩枝的蘋果小枝被噴灌_獮混 合物(0. 02¾活性成份)到滴點,24小時之後,接 種徽菌conidi a懸浮物。植物在相對大氣灞度9 0到1 0 0先 下培餐5天,在20到24TC溫室内再保持10天。接種 15天後評估威染斑點。表1, 2或3之大部份式I化合 -98- 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) I------^ I装------訂----γ、-線 (請先閱讀背面之注意事項再填寫本頁) A7 304860 B7__ 五、發明説明(p) 物對斑點疾病具持鑲性活性。 (請先閲讀背面之注意事項再填寫本頁) 實例B — 8 :對大麥Erysiphe graiinis之活性 a )殘留保護活性 約8公分高的大麥植物被喷漏水性喷灑混合物 (0. 02%活性成份)到滴黏,3到4小時後,喷上撤 菌 conidia。接種植物被置於22Ό»室,接種後1 〇天 進行評估徽菌戚染。 b )条統活性 將水性嗦钃混合物(0. 002%活性成份,相對於 土壤體積)倒入約8公分离之大麥植物四颺。小心避免嗔 钃混合物與任何地面上的檀物接觸。48小時之後•對植 物接種conUia徽菌懸浮物。接種植物被置於2 2*0粗室内 。接種後10天,評估徽豳感染。式I化合物,特別是 1.117, 2. 24和3. 24等化合物一般能将疾病 降低到20%,在某些情況下能完全避免。 經濟部中央樣準局貞工消費合作社印製 實例8_9 :辑篇果小枝Podosphaera leucotricha之活性 含約15公分新鮮嫩枝的蘋果小枝被噴漏喷灑混合物 (0. 06%活性成份),24小時之後,受處理之植物 被接種徽菌conidi a懸浮物,置於相對大氣濕度7 0%及 201C的控制琛境下。接種1 2天後評估徽菌戚染。式I 活性成份讓疾病減少到小於2 0%。對照組植物的疾病戚 染率為1 0 0 %。 實例Β — 1 0 :對蘋果Botrytis cinerea之活性.殘留保 -99- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央揉準局貝工消费合作社印裝 A7 B7 五、發明説明(fa) 護活性 用噴鱺混合物(〇. 02%活性成份)投與故意破壤 蘋果之傷口.經過處理之蘋果接著被接鬌徽豔孢懸浮物, 並在高大氣濕度和約201培蓍一遇。試驗物霣的殺徽豳 活性僳從傷口呈腐烟I的數目而決定。式I活性成份能典I滅 缓傷口腐_Μ延,某些情況下能完全阻止。 實例 Β - 1 1 :對 Helainthosporiun graiineu·活性 小麥種子被徽茵孢懸浮物汙染•讓其乾燦。被汙染種 子被包敷試驗物質(600ppm活性成份,相對於種子 重董)的懸浮物。2天後,將種子安排在合適的含瓊脂的 皿中,再過4天後,評估種子四周徽醣菌落發展情況。依 徽菌®落數目和大小評估試驗物質。在某些情況下,某些 式I化合物顯示優良活性,也就是抑制徽»菌落的活性。 實例 B - 1 2 :對胡瓜 Colletotrichu· lagenariu·之活性 生長2遇之胡瓜植物被噴漏噴灌混合物(濃度0. 0 025) 。 2天後,該植物被接種徽菌孢懸浮物(1. 5 X 1 0s抱子/毫升),在23t!及高大氣濕度下培餐3 6小時。繼鑛在一般大氣濕度下及22-231培餐。接 種後8天評估徽_越染發展情況。未處理而被絨染的對照 组植物的徽菌威染率達1 00%。 在某些情況下,式I化合物,待別是1. 5和3. 24 化合物能完全抑制威染疾病。 實例Β - 1 3 :對裸麥Fusariu· nivale之活性 -100- 本紙張尺度逋用中國國家標準(CNS ) A4規格(210X297公嫠) --;-------^ .装------訂-----球 (請先閲讀背面之注意事項再填寫本頁) 304860 A7 B7 五、發明説明(fjr) 使用混合滾苘将試驗殺徽@_包敷被Fusairiu· nivale 天然性越染之裸麥 cv.Tetrahell ,並使用以下濃度·· (請先閲讀背面之注意事項再填寫本頁) 20或6 ppm活性成份(相對種子重蛋)。 使用播種機在10月份播種受戚染和經處理的裸麥, 播種地為3米,有6種子,每種濃度重覆3次。 試驗植物在正常耕地條件(較佳為冬季月份能完全予 以覆蓋的匾域)生長,直到評估鉞染為止。 為了評估植物毒性,在秋天計算種子發芽數目,在春 天記錄每單位面稹之植物數目/每株植物的發芽數。 為了決定活性成份之活性.融雪之後馬上測定被 Fusariu·威染植物的百分率。就本例而言,受威染植物的 數目小於5%。發芽的植物擁有健康的外觀。 實例B - 1 4 :對小麥Septoria nodoru·之活性. 生長到3片葉子陏段的小麥被嗔漏製備於活性成份( 2. 8 : 1)的可獮濶粉末喷灑混合物(60ppm活性 成份)。 經濟部中央標準局員工消費合作社印製 2 4小時之後,經過處理的植物被接種徽囍(:〇|^|11&amp;懸 浮物。接著該植物在相對大氣濕度為90 — 1 00¾之下 培養2天,並置於20 — 2424溫室10天。接種13 天後,評估徽®烕染,小麥植物受威染比例小於1%。 實例B- 1 5 :對稻米Rhizoctonia solani之活性 局部保護土壤應用 對生長10天稻米植物四周土壤澆以懸浮物(嗔躍混 -101- 本紙張尺度逋用中國國家標準(CNS ) A4規格(210X297公釐) ________B7_ 五、發明説明( ·該戀浮物供製備於讕配的試驗物質,不使地面上 植物輿想浮物接觸。3天後,將被Rhizoctonia solani成 麥稻莖部接種於每軀花盆之稻米植物之閩。在白天 2 9t!及夜晩2 61D及相對大氣嫌度9 5%之控制琛塊下 培餐6天,評估徽菌戚染情況。结果小於5%之稻米植物 被感染,植物的外觀健康。 局部保護藥子匾用 生長12天的稻米植物被嘖灑讕配之試驗物質所製備 的懸浮物。1天後,將被Rhizoctonia solaniii染的大麥 莖部置於每偏花盆的稻米植物之間而進行接種。在白天 2 及夜晩2 6¾及相對大氣灞度9 5%之控制環境下 培養6天,開始評估植物。未經處理而被接種的對照组植 物的徽菌威染率高逹100%,在某些情況下,式I化合 物會完金抑制疾病的EC染。 B .殺昆典活性 實例 B — 1 6 :對豆蚜(A p h i s c r a c c i v 〇 r a )活性 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再填寫本頁) 豌豆苗被豆蚜絨染之後,接著被含有 400p pm 活性成份的喷鼸混合物處理,在20t:培養。在3天和6 天之後加以評估。此試驗中,表1到7的化合物具備優良 的活性。特別是化合物4. 5之異構物活性超«80%。 實例 B - 1 7 :對條蕖甲(Diabrotica balteata)活性 幼玉米植物被哦以含有4 0 0 p pm活性成份的水性 乳液噴灑混合物,在嘖濯塗靥乾燥之後•該大豆植物被敝 -102- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 經濟部中央標準局員工消費合作杜印製 A7 B7 五、發明説明(γ) 佈植物被散佈第二階段的1〇餹條蕖甲幼龕並置入一鵪塑 謬容器,在6天之後才開始進行評估。族群數目減少百分 率(活性%)乃經由比較接受處理死亡的幼巔和入料損失 與未經處理植物而獲得。在試驗中,表1到7化合物都具 備優良的活性。待別是化合物1. 5, 1.24, 2. 24. 3. 24, 4. 5的異構物1, 414的異構 物1,4. 14的異構物1,4. 117的二異構物, 4· 121. 4. 170· 5. 9 的異構物 1 和 5. 51 的異構物1之活性离於80%。 實例B— 1 8 :對美洲菸夜蛾活性 幼大豆物被噴以含有4 0 0 p pm活性成份的水性乳 液噴灑混合物,在喷灑塗層乾燥之後,該大豆植物被散佈 於10侮第一幼巖階段美洲菸夜蛾,並置入一塑腰容器, 在6天之後才開始進行評估。族群數目滅少百分率(活性 %),或者是入料損失,乃經由比較接受*理舆未經處理 植物的死亡甲典和入料損失而獲得。在試驗中,表1 一 7 化合物都具備優良的活性。待別是化合物 4. 5的異構 物1, 4. 14的異構物1, 4. 18, 4. 117的 二異構物,4. 121, 5. 9的異構物1和5. 52的 異構物1之活性超遇8 0%。 實例B — 1 9 :對斜紋斑蛾(Spodoptera littoralis)之活 性 幼大豆物被喷以含有4 0 〇 p Pm活性成份的水性 -103- 本紙張尺度適用中國國家橾準(CNS ) Α4規格(210X297公釐) I.------&gt;-*--—裝------訂-----線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央樣準局員工消費合作社印製 層乾嫌之後,該大豆植物被散 斜紋斑蛾,並置入一塑腰容器 估。族群數目減少百分率(活 乃經由比較接受處理舆未經處 失而獲得。在試驗中,表1 一 。特別是化合物4 . 5的異構 • 5. 1.24.2.24, 5之異構物1, 5. 9之異構 之活性超遇8 0%。 (Tetranychus uriticae)之活 蛛之混合物,於1天後,被喷麵 水 性 乳 化 噴 濯 混 合 物 » 在 2 5 族 群 減 少 百 分 率 ( % 活 性 ) 你 卵 » 幼 襄 和 成 鑫 數 巨 而 澜 定 的 物 都 具 備 優 良 的 活 性 〇 特 別 是 2 • 2 4 3 • 2 4 % 4 • 5 物 1 • 4 • 1 1 7 的 二 異 5 5 2 的 異 構 物 1 之 活 性 超 us licroplus的活性 PVC板上,用楠毛球覆Μ之 104- 304860 五、發明説明(7$) 乳液喷漏混合物,在喷灑塗 佈於10值第三幼蠱陽段之 ,在6天之後才鬭始進行評 性%),或者是入料損失, 理植物的死亡甲鑫和入料損 7化合物都具備優良的活性 物1, 4. 14的異構物1 3 . 24,4. 18,4. 物1和5. 52之異構物1 C .殺恙蟲活性 實例B—20:對棉紅蜘蛛 性 幼豆植物被散佈棟红蜘 含40 0 p pm活性成份之 培餐6天,接着進行評估。 比較經處理及未處理之死亡 。在試驗中,表1— 6化合 化合物1. 5, 1. 24, 的異物1, 4.14的異構 構物,5. 9的異構物1和 遇 8 Ο %。 實例 B-2 1 :對 Boopohil 吸飽的11性成虱被置於 A7 B7 -'^ 装 訂 *線 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) A7 B7 五、發明説明(# ,將含1 2 5 P pm活性成份的水性試驗溶液锔入覆蓋成 虱。取走棉毛球,培餐4遇供産卵。不管是雌性的死亡率 或存活率,或者是對卵的殺卵活性,其活性很明顯。 _龜 一 / I 一,-線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 -105- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐)The spore suspension of Phy tophthora inf estans. The plant was then placed in a sprinkler irrigation room with a saturated humid atmosphere from 18 to 2 Ot: for 5 days. After that, a typical leaf spot was developed, and the number and size of the test specimens were used to evaluate the -94- This paper scale is applicable to the Chinese National Standard Falcon (CNS) A4 specification (210X297 mm) 304860 A7 B7 V. Description of the invention u?) active. The untreated but infected plants in the control group showed a 100% dyeing rate, and those who used one of the active ingredients of formula I in the table, especially made 1. 5 • 1. 24, 1. 117, 2. 24 , 2. 74 and 3. 2 4 compounds, the infection rate of the above two groups of tests was reduced to 20% or less. Example B-2: Plasiopara viticola (Bert. Et C ur t.) (B er 1. et D e T ο ni) activity (a) residual preventive activity «Grape branch cv. &Quot; Chassels” in the greenhouse Medium growth, when it grows into a 10-leaf stage, 3 plants among them_pre-mix (active ingredient of 200p pm). After the coating on the plants is dried, the emblem_spore is evenly implanted on the bottom of the medicine. Float. The plant was then kept in the wet room for 8 days. After that, the control plant had developed disease. The number and size of damaged parts of the treated plant were used to evaluate the activity of the test substance ) Therapeutic activity Printed by the Employees Consumer Cooperative of the Central Standards Bureau of the Ministry of Economy (please read the precautions on the back and then fill out this page) Grape twigs CV. ”Chassels” grow in the greenhouse, when they grow into 10 leaves, the bottom of the leaves Spray the spore suspension of Plasiopara viticola. After the plant is placed in the humid room for 24 hours, spray the active ingredient mixture (200 ppm of active ingredient). Then keep the plant in the humid room for 7 days. After that, the control plant Already The disease clearly developed. The number and size of the damaged parts of the treated plants were used to evaluate the test -95- This paper scale is applicable to the Chinese National Standard (CNS) Λ4 specification (210X297 mm) Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Printed A7 B7__ V. Description of the invention (? Called the activity of the test substance. Compared with the plants in the control group, the dyeing rate of the active ingredients of Formula I is 20% or less. Example B-3: For beets ( B etavu 1 garis) P ythiudebaryanu's active microbes grow on the sterilized oatmeal and add it to the mixture of soil and sand. Put this soil into the flowerpot and plant sugar beets. After planting, immediately The test product formulated as Coba® powder was poured into the soil in the form of water-based floats (20p pm active ingredient, relative to soil mother). The flower pot was placed at a temperature of 20 to 24Ό for 2 to 3 logic. The two stubble sprays water to keep the soil evenly moistened. The evaluation is carried out to calculate the number of beet plant sprouts and the number of healthy and infected plants. (B) Active emblem after seed coating_oats in disinfection Grow on top, add it to the mixture of soil and sand. Fill this planted soil into flower pots and plant it with a seed powder (100 ppm active ingredient, relative to the weight of the seed). Preparation of sugar beet. Flower pots and seeds are placed in a greenhouse at 20-24C for 2 to 3 passes. Gently spray water to keep the soil evenly moist. When evaluating, calculate the number of beet plant buds and key health Number of infected plants. Treated with the active ingredients of formula I, except for the compounds 1. 5, 1. 24, 1. 117, 2. 24, 2. 74 and 3. 24. Over 80% of the plants germinate and have a healthy appearance. Among the flower pots in the control group, only a few plants with unhealthy appearance germinated. -9 6 _ This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) I .------------ 、 玎 ----- ^ (Please read the note on the back first Please fill in this page again) A7 B7 304860 V. Description of the invention (7 /) Example B — 4: Residual protective activity against Cercospora arachidicola of groundnuts 10 to 15 g. The groundnuts separated by the “water-based water-spilling mixture (. 02% active ingredient) until it becomes sticky, and 48 hours later, it is implanted into the spore suspension of the top of the emblem sugar. Plants were bred in 2 1 t: and high tidal flat atmosphere for 72 hours and then placed in the greenhouse until the typical leaf spots appeared. After inoculation, the activity of the active ingredient is evaluated by the number and size of drug spots. The active ingredient of formula I makes the leaf spot occupy less than 10% of the leaf area. In some cases, the disease is almost completely eliminated (0-5% infection). Example B-5: Activity on wheat Puccinia graiinis a) Residual protective activity After 6 days of planting, the wheat plant was sprayed to the dropping point with an aqueous spray yaya compound (0.002 active ingredient). After 24 hours, the emblem was inoculated Zhongzhi 111: 0111〇3? (^ 0 suspension. After 48 hours of cultivation (condition is 2〇10, relative humidity 95 to 100%), the plants are placed in a ffl room at 22 * C, inoculated for 12 days Then evaluate the development of embroidered blisters. B) After 5 days of active planting, pour the water-based sprinkler irrigation mixture (0.006% active ingredient, which is sharper than the soil accretion) into the surrounding wheat plants. Be careful to avoid the subsequent mixture coming into contact with any plants on the ground. After 48 hours, the plants were inoculated with ureidospore suspension suspension. After 48 hours of inoculation (conditions 20TC, relative humidity 95 to 100%), place the plants in a rough room. Twelve days after the inoculation, the development of _blisters was evaluated. -97- The size of this paper is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) 丨 ^ ------ "I installed ------ order ----- ^ line (please read the back first Please pay attention to this page and fill out this page) Printed by the Central Sample Bureau of the Ministry of Economic Affairs of the Beigong Consumer Cooperatives of the Ministry of Economic Affairs Printed by the Central Consumer Agency of the Ministry of Economics A7 ___B7__ 5. Description of the invention) Compounds of formula I, especially 1. in Table 1 , 1.24, 1. 11 7, 2. 74 and other compounds significantly reduced Hui Zhao Qi Ran, in some cases reduced to 10-0%. Example B-6: Activity on rice Pyricularia oryzae a) Residual prevention active rice After the plant grows for 2 encounters, it is sprayed with water-based deer compound (0.02% active ingredient 0 to the dropping point. After 4 to 8 hours, it is inoculated with the floating partridge conidi a to float. After 5 days of inoculation, the infection of the mackerel is evaluated. During this period, the relative intensity is maintained at 95 to 100%, and the temperature is 22 &quot; C. B) The system activity is poured on the water-based water-spraying mixture (0.006% active ingredient, relative to the soil lumps) and grown around the 2 rice. Careful Avoid spraying the mixture with any plants on the ground. Then put the pots in the quantity so that the stem of the rice is the lowest Water into it. 9 After 6 hours, the plants are inoculated with conidi a microbe suspension and kept at a relative humidity of 95 to 100% and a temperature of 241C. In many cases, the compound of formula I prevents infection The condition of the plant deteriorates. Example B-7: Residual retention activity on apple Venturia inaequalis Apple twigs containing fresh tender shoots of 10 to 20 cm are sprayed with _ 狝 mixture (0.022 active ingredient) to the drop point, 24 hours later, inoculated Suspended suspension of anisobacteria conidi a. Plants were first cooked for 5 days at a relative atmospheric temperature of 90 to 100, and then kept in a greenhouse at 20 to 24TC for another 10 days. After 15 days of inoculation, the infection spots were evaluated. Table 1, 2 Or most of the 3 types of I compound-98- This paper scale is applicable to China National Standard (CNS) Α4 specification (210X297 mm) I ------ ^ I installed ------ order ---- γ, -line (please read the precautions on the back before filling out this page) A7 304860 B7__ V. Description of the invention (p) The substance has a mosaic activity on spot diseases. (Please read the precautions on the back before filling out this page) Example B-8: Activity against barley Erysiphe graiinis a) Barley plants with residual protective activity of about 8 cm Spray the water-based spray mixture (0.02% active ingredient) to the drop, and after 3 to 4 hours, spray the conidia to withdraw bacteria. The inoculated plants are placed in the 22Ό »room, and the infection is evaluated 10 days after inoculation. B) Systemic activity: Pour the water-based mixture (0.002% active ingredient, relative to soil volume) into the barley plant Siyang about 8 g. Be careful to avoid contact with any sand objects on the ground. After 48 hours • Inoculate plants with conUia microbe suspension. The inoculated plants are placed in a 2 2 * 0 rough room. Ten days after the inoculation, the infection of Huibin was evaluated. Compounds of formula I, especially compounds such as 1.117, 2. 24 and 3. 24, can generally reduce the disease to 20%, and in some cases can be completely avoided. Printed by the Ministry of Economic Affairs of the Central Bureau of Samples of the Jungong Consumer Cooperative 8_9: Compilation of the activity of the fruit twigs Podosphaera leucotricha The apple twigs containing about 15 cm of fresh tender shoots were sprayed with a mixture (0.06% active ingredient), 24 hours Afterwards, the treated plants were inoculated with the suspension of the fungus conidi a and placed under the control of 70% relative humidity and 201C. Twelve days after the inoculation, the infection of the microbes was evaluated. Formula I active ingredients reduce disease to less than 20%. The disease infection rate of plants in the control group was 100%. Example Β — 1 0: Activity on Apple Botrytis cinerea. Residual guarantee -99- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) Printed by the Ministry of Economic Affairs Central Bureau of Industry and Commerce Beigong Consumer Cooperative A7 B7 5. 3. Description of the invention (fa) The spraying mixture for active protection (0.02% active ingredient) is administered to the wound of deliberately breaking apples. The treated apples are then taken up by the suspension of the spores of Corydalis angustifolia. 201 Pei-Yu encounter. The antimicrobial activity of the test sample was determined by the number of decay I in the wound. The active ingredient of formula I can reduce the wound decay _M extension, in some cases it can be completely prevented. Example Β-1 1: Active against Helainthosporiun graiineu · Wheat seeds are contaminated with suspended solids of the spores of the microbe. Let them dry. Contaminated seeds are coated with a suspension of the test substance (600 ppm active ingredient, relative to seed weight). After 2 days, arrange the seeds in a suitable dish containing agar, and after 4 days, evaluate the development of the sugar colonies around the seeds. The test substance was evaluated according to the number and size of Anhui bacteria® colonies. In some cases, certain compounds of formula I show excellent activity, i.e., the activity of inhibiting the colonies of the emblem. Example B-12: Activity against courgettes Colletotrichu · lagenariu · The courgette plants grown in 2 encounters were sprayed with sprinkler irrigation mixture (concentration 0.025). After 2 days, the plant was inoculated with a suspension of anisobacteria spores (1.5 x 10 spores / ml), and the meal was cultivated at 23 t! And high atmospheric humidity for 36 hours. Following the mine under normal atmospheric humidity and 22-231 meals. The development of Hui_Yueran was evaluated 8 days after seeding. The control group of untreated but velvet-stained plants had an infection rate of 100%. In some cases, the compounds of formula I, except for 1.5 and 3.24, can completely inhibit infection. Example Β-1 3: Activity on rye Fusariu · nivale-100- This paper scale uses the Chinese National Standard (CNS) A4 specification (210X297 male daughter)-; ------- ^ .Package- ---- order ----- ball (please read the precautions on the back before filling in this page) 304860 A7 B7 Fifth, the invention description (fjr) Use the mixed roller to kill the test emblem @_ 包装 被 Fusairiu · nivale Naturally dyed rye cv. Tetrahell, and use the following concentrations ... (please read the notes on the back before filling this page) 20 or 6 ppm active ingredient (relative to seed heavy egg). The seeded and treated rye was sown in October using a planter. The planting area was 3 meters, with 6 seeds, and each concentration was repeated 3 times. The test plants were grown under normal cultivated land conditions (preferably plaque fields that could be fully covered in the winter months) until evaluation of the contamination. To assess phytotoxicity, the number of seeds germinated was calculated in the fall, and the number of plants per unit of lentinella per plant was sprouted in the spring. In order to determine the activity of the active ingredient, the percentage of plants infected with Fusariu · wei was determined immediately after melting the snow. For this example, the number of infected plants is less than 5%. Germinated plants have a healthy appearance. Example B-1 4: Activity against wheat Septoria nodoru. Wheat grown to three leaves is prepared from a sprayable mixture of active ingredients (2.8: 1) in a powdery sprayable powder (60 ppm active ingredient) . After printing for 24 hours by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, the treated plant was inoculated with the emblem (: 〇 | ^ | 11 &amp; suspended matter. Then the plant was cultivated under a relative atmospheric humidity of 90-1 00¾ 2 Days, and placed in a greenhouse from 20 to 2424 for 10 days. After 13 days of inoculation, the Hui® is stained, and the proportion of wheat plants affected by the infection is less than 1%. Example B- 1 5: Active protection of rice Rhizoctonia solani Local application of soil for growth Suspended soil is poured around the soil around the rice plants for 10 days (嗔 跃 混 -101- This paper scale adopts the Chinese National Standard (CNS) A4 specification (210X297 mm)) ________B7_ V. Description of the invention (· The love float is for preparation The test substance is matched so that the plants on the ground do not come into contact with floating objects. After 3 days, the stems of Rhizoctonia solani's wheat-growing rice will be inoculated into the rice plant in each flower pot. During the day 2 9t! And nightfall 2 61D and the relative atmospheric suspicion 95% control the food under the Chen block for 6 days to evaluate the infection of the fungus. The result is that less than 5% of rice plants are infected and the appearance of the plant is healthy. The local protective medicine plaque is grown for 12 days Rice plant Suspend the suspension prepared by the test material. After 1 day, place the stems of barley infected with Rhizoctonia solaniii between the rice plants in each partial pot for inoculation. During the day 2 and nightfall 2 6¾ and The plants were cultured for 6 days in a controlled environment at a relative atmospheric temperature of 9 5%, and the plants were evaluated. The control group plants inoculated without treatment had a high infection rate of 100%. In some cases, the compound of formula I would Finished gold inhibits the EC infection of the disease. B. Example of killing Kun Dian activity B — 1 6: Printed on bean aphid (A phiscracciv 〇ra) Active Ministry of Economy Central Standards Bureau employee consumer cooperatives (please read the notes on the back before filling in This page) Pea seedlings were dyed by the bean aphid down, then treated with a spray-emulsion mixture containing 400p pm active ingredient, at 20t: incubation. After 3 days and 6 days were evaluated. In this test, the compounds of Tables 1 to 7 Has excellent activity. Especially the isomer of compound 4.5 has an activity exceeding «80%. Example B-1 7: Diabrotica balteata active young corn plant quilt contains 4 0 0 p pm active ingredients Water-based emulsion spray mixing After the coating is dried, the soybean plant is covered by -102- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm). The consumer cooperation cooperation of the Central Standards Bureau of the Ministry of Economic Affairs is printed by A7 B7. 5. Description of the invention (γ) Cloth plants were scattered in the second stage of the 10th noodles niche and placed in a quail container, and the evaluation was started after 6 days. The percentage reduction in the number of ethnic groups (% of activity) was obtained by comparing the apex that died under treatment and the feed loss with untreated plants. In the test, the compounds of Tables 1 to 7 all had excellent activities. Wait for the compounds 1. 5, 1.24, 2. 24. 3. 24, 4. 5 isomers 1, 414 isomers 1, 4. 14. isomers 1, 4. 117 isomers The activity of Isomer 1 of 4.121. 4. 170 · 5.9 and Isomer 1 of 5.51 are 80%. Example B-18: The active young soybeans of American cotton budworm were sprayed with an aqueous emulsion spraying mixture containing 400 ppm active ingredients. After the spray coating was dried, the soybean plant was scattered on 10 In the larval stage, the American tobacco budworm, placed in a plastic waist container, was evaluated only after 6 days. The percentage of population reduction (activity%), or feed loss, is obtained by comparing acceptance * of the death of untreated plants and feed loss. In the test, the compounds in Tables 1 to 7 all had excellent activities. To be distinguished is the isomer of compound 4.5, the isomer of 1.14, the diisomer of 4.18, 4.117, the isomers of 4.121, 5.9 is 1 and 5. The activity of 52 isomer 1 exceeded 80%. Example B — 19: Active young soybeans of Spodoptera littoralis are sprayed with water-103 containing 40 〇p Pm active ingredient- This paper scale is applicable to China National Standard (CNS) Α4 specification (210X297 Mm) I .------ &gt;-* --— install ------ order ----- line (please read the precautions on the back before filling in this page) After the printed layer of the consumer cooperative of the bureau employees was suspected, the soybean plant was spotted and spotted into a plastic waist container. Percentage reduction in the number of ethnic groups (living is obtained by comparison with the treatment and without loss. In the test, Table 1 I. Especially the isomerization of compound 4.5 • 5. 1.24.2.24, the isomer of 5, 5. The heterogeneous activity of 9 is over 80%. The mixture of live spiders (Tetranychus uriticae) is sprayed with water-based emulsified spray mixture after 1 day »Reduced percentage in 2 5 ethnic groups (% activity) of your eggs »Youxiang and Chengxin both have excellent activity. Especially 2 • 2 4 3 • 2 4% 4 • 5 compounds 1 • 4 • 1 1 7 isomers 5 5 2 isomers The activity of the substance 1 is super active on the active PVC board of us licroplus, covered with the wool ball 104-304860 V. Description of the invention (7 $) The emulsion spray mixture is sprayed on the 10th third young Guyang section In other words, the evaluation was not started until 6 days later), or the feed loss, the death of the plant and plant, Jiaxin and the feed loss 7 compounds have excellent actives 1, 4. 14 isomers 1 3 . 24,4. 18,4. Isomer 1 and 5. 52 isomer 1 C. Chiggericidal activity example B— 20: The cotton red spider sex young bean plants are spread with red spiders containing 40 ppm active ingredients for 6 days, and then evaluated. Compare treated and untreated deaths. In the test, Tables 1 to 6 are compound 1. 5, 1. 24, foreign matter 1, 4.14 isomer, 5. 9 isomer 1 and encounter 8 Ο%. Example B-2 1: 11 sex adults full of Boopohil are placed in A7 B7-'^ binding * line (please read the precautions on the back before filling this page) This paper size is applicable to the Chinese National Standard (CNS) Α4 specification (210X297mm) A7 B7 5. Description of the invention (#, the aqueous test solution containing 1 2 5 P pm active ingredient is covered into adult lice. The cotton wool ball is removed, and the meal is prepared for spawning. Whether it is female or not The mortality or survival rate, or the egg-killing activity on eggs, the activity is very obvious. _ 龟 一 / I one,-line (please read the precautions on the back before filling this page) Employee consumption of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the cooperative-105- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm)

Claims (1)

A8A8 C3 ΗC3 Η A R3 物 1 合-R 混(-物 Ν 構 或 , 異和 1 1 其子 1 和 I , 原 R H R 物氮 ο C ο 構為為為為 異 X Υ X Υ 其丨 ) 及 a b 中 其 (請先閱讀背面之注意事項再填寫本頁) .f 2 R 或 中 其 訂 經濟部中央橾準局負工消費合作社印裝 ; 或 基氫 烷為 } ) ..-/ 4 4 4獨基cC C § 4 _ I I 個 R 1 1 1 3 N C 1 或丨 (R 子., 為和原氫 1 2 氧為 1 -為 1 2 R R A R 基 R 硫 基 氫 為 CA R3 compound 1 is mixed with -R mixed (-compound N configuration or, hetero and 1 1 its sons 1 and I, the original RHR compound nitrogen ο C ο is configured to be hetero X Υ X Υ qi) and ab which ( Please read the precautions on the back before filling out this page). F 2 R or the printed version of the Ministry of Economic Affairs Central Bureau of Preservation Consumer Cooperatives; or the base is}) ..- / 4 4 4 single base cC C § 4 _ II R 1 1 1 3 NC 1 or 丨 (R sub., Is and the original hydrogen 1 2 oxygen is 1-is 1 2 RRAR group R thiol hydrogen is C 基基 Z 烷烷Alkyl Z alkane B C 基 烷 -SJ/ 4 C 甲 或 基 氰 基 丙 璟 基 丙 環 η η 素 鹵 為 ί 其, ’ 基 者氧 同烷 不 } 或 + 同 C 相 -為 1 基基 C 吩 D -噻 , 或 基 C 本紙張尺度適用中國國家揉準(CNS ) Α4規格(210X297公嫠) C 2 C 烷 \J/ , 4 基 C 烷 I 鹵 申請專利範圍 C i — C 2 )鹵烷氧基 C C4 )次烷基二氧棊 η 為◦,1 ,2 或 3 ; Ζ 為—◦ -,一 0 — (Ci — C4 )烷基—, —(Ci — C 4 )院基—0 —,— S ( 0 ) 2 — &gt; S B為(Ci _C6 )烷基,鹵一 (C C 4 )烷基 ,(C 5 - C 6 )環烷基,或為(C2 _C6 )_基或 (C 2 - C 4 )炔基一(Ci - C 2 )烷基,每個未被取 代或被1到3個鹵原子取甙,或為苯基,其未被取代或被 (C 1 — C3 )烷基,鹵素一(Ci - C 6 )烷基,鹵素 取代,或為 R (CH)BC alkyl-SJ / 4 C methyl or cyano cyanopropyl propyl ring η η element halide is ί, 'group of oxygen is the same as alkane} or + the same C phase-is a 1 group C phen D-thio, Or base C This paper scale is applicable to China National Standard (CNS) Α4 specification (210X297 public daughter) C 2 C alkane \ J /, 4 base C alkane I Halogen patent application scope C i — C 2) haloalkoxy C C4 ) Hypoalkyldioxane η is ◦, 1, 2 or 3; ZO is —◦-, a 0 — (Ci — C4) alkyl —, — (Ci — C 4) courtyard group — 0 —, — S (0) 2 — &gt; SB is (Ci _C6) alkyl, halo- (CC 4) alkyl, (C 5-C 6) cycloalkyl, or (C2 _C6) _ group or (C 2-C 4) alkynyl mono (Ci-C 2) alkyl, each unsubstituted or substituted with 1 to 3 halogen atoms, or phenyl, which is unsubstituted or (C 1-C3) alkyl, Halogen- (Ci-C 6) alkyl, substituted with halogen, or R (CH) Rg R8 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局貝工消費合作社印製 或三甲基甲矽烷基; R 5 ,Rs和{?9個自獨立為氫,(Ci -C4 )烷 基,和 Rs和R7為氬或鹵素; R 3為氫,(C ! — C s )烷基 &gt; 含1到5個鹵原子· 的(Ci — Cs )鹵烷基* ( C 1 — C4 )烷氧基一(Ci -C 2 )烷基,(C2 - C4 )烯基,其係未被取代或被 1到3個鹵原子取代,(C2 — C4 )炔基,未被取代或 被1到2個鹵原子取代的環丙基甲基,氰基一(Ci—C^ 烷基;(C! —C4 )烷氧基羰基一 (C! — C2 )烷基 -2- 本紙張尺度適用中國國家梂準(CNS ) A4说格(210X297公釐) • ▲ Λ Α8 304860 Bd D8 六、申請專利範圍 ’苯基一 (C ! — C 2 )烷基,其係未被取代或被鹵素, (Cl - C 4 )鹵烷基,未被取代的苯基或被個自獨立被 (C 1 - C 4 )烷基,(Ci - C 4 )烷氧基,鹵素,含 1到3個鹵素原子的(c i _ C 2 )鹵烷基,硝基單取代 或二取代的苯基,或未被取代的吡啶基或被含1到3個鹵 素原子的(C i — C 2 )鹵烷基或硝基取代的毗啶基; R4為(C! - C 4 )烷基,苯基,或 R3和R4 —起與其所鍵结的氮原子形成4 — (1 , (請先閱讀背面之注意事項再填寫本頁) 2 ,4 一三唑基),4 一碼啉基或吖庚因基;以下化合物 除外 αRg R8 (Please read the precautions on the back before filling this page) Printed or trimethylsilyl by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs; R 5, Rs and {? 9 are independently hydrogen, (Ci -C4) alkyl, and Rs and R7 are argon or halogen; R 3 is hydrogen, (C! — C s) alkyl> (Ci — Cs) haloalkyl * containing 1 to 5 halogen atoms * ( C 1-C4) alkoxy mono (Ci-C 2) alkyl, (C 2-C 4) alkenyl, which is unsubstituted or substituted by 1 to 3 halogen atoms, (C 2-C 4) alkynyl, un Cyclopropylmethyl substituted or substituted with 1 to 2 halogen atoms, cyano- (Ci-C ^ alkyl; (C! -C4)) alkoxycarbonyl- (C! -C2) alkyl-2 -This paper scale is applicable to China National Standard (CNS) A4 grid (210X297mm) • ▲ Λ Α8 304860 Bd D8 VI. Patent application scope 'phenyl mono (C! — C 2) alkyl, which is not Substituted or halogenated, (Cl-C 4) haloalkyl, unsubstituted phenyl or independently substituted (C 1-C 4) alkyl, (Ci-C 4) alkoxy, halogen, containing (Ci _ C 2) haloalkyl with 1 to 3 halogen atoms, nitro Substituted or disubstituted phenyl, or unsubstituted pyridyl or pyridyl substituted with (C i — C 2) haloalkyl or nitro containing 1 to 3 halogen atoms; R4 is (C!- C 4) alkyl, phenyl, or R3 and R4 together with the nitrogen atom to which they are bonded to form 4 — (1, (please read the precautions on the back before filling this page) 2, 4-triazolyl), 4 A quinolinyl or azepine group; except the following compounds α 訂 經濟部中央揉準局貝工消费合作社印製 2 ·如申請專利範圍第1項的式I化合物,其中 X為氮和 Υ 為 0 C Η 3 。 3 ·如申請專利範圍第1項的式I化合物,其中 X 為 C Η。 4 ·如申請專利範圍第1項的式I化合物,其中 X為氮, Υ為N H C Η 3和 只1為只,(:幵3 ,環丙基或CN。 -3- 本紙張尺度逍用中國國家梂準(CNS ) A4^ ( 210Χ297公嫠) 經濟部中央梂準局男工消費合作社印製 A8 B8 C8 D8六、申請專利範圍5 ·如申請專利範圍第2到4項中任一項的式I化合物, 其中 A為氧,NCH3或正C6Hs 。 6 ·如申請專利範圍第2到4項中任一項的式I化合物, 其中Ri為,氫,甲基,環丙基或氰基。 7 ·如申請專利範圍第2到4項中任一項的式I化合物, 其中Ri為(C! 一 C4 )烷基或環丙基。 8 ·如申請專利範圍第2到4項中任一項的式I化合物, 其中R 2為 · 和 \=^A(d) η D基為齒素’ (Cl _C4 )院基,(Cl — C 4 ) 烷氧基,被1到5個鹵原子取代的(C ! 一 C 2 )烷基, (Ci - C 2 )鹵烷氧基,(Ci - C 4 )次烷基二氧基 ,氟基或硝基,或噻吩基;和 η 為 0,1 ,2 或 3。 9 ♦如申請專利範圍第2到4項中任一項的式I化合物, 其中 R 2 為 Ζ·Β-&lt; 5 - ( D ) η Ζ 為一Ο —,一〇一(Ci — C4)院基 一,一(Ci —C4)烷基一〇一,一 S(0)2 —。 1〇·如申請專利範圍第1到4項中任一項的式I化合 物,其中R 2為 -4 - (請先閱讀背面之注意事項再填寫本頁) 訂Printed by Beigong Consumer Cooperative of the Central Bureau of Economic Development of the Ministry of Economic Affairs 2 · For example, the compound of formula I in item 1 of the patent application, where X is nitrogen and Υ is 0 C Η 3. 3. A compound of formula I as described in item 1 of the patent scope, wherein X is C Η. 4 · For example, the compound of formula I in item 1 of the patent application, where X is nitrogen, Υ is NHC Η 3 and only 1 is only ((幵 3, cyclopropyl or CN. -3- This paper scale is used in China CNS A4 ^ (210Χ297 公 嫠) Printed A8 B8 C8 D8 by the Central Bureau of Economic Affairs of the Ministry of Economic Affairs of the Male Workers ’Cooperatives of the People's Republic of China. 6, Patent application scope 5 · For any of the items 2 to 4 A compound of formula I, wherein A is oxygen, NCH3 or n-C6Hs. 6 A compound of formula I according to any one of claims 2 to 4, wherein Ri is hydrogen, methyl, cyclopropyl or cyano. 7 · As in the patent application, any one of items 2 to 4 of formula I compound, wherein Ri is (C!-C4) alkyl or cyclopropyl. 8 · As in any of the patent application, items 2 to 4 The compound of formula I in the item, wherein R 2 is · and \ = ^ A (d) η D group is a dentin '(Cl _C4) yard group, (Cl — C 4) alkoxy group, is substituted with 1 to 5 halogen atoms Substituted (C!-C 2) alkyl, (Ci-C 2) haloalkoxy, (Ci-C 4) hypoalkyldioxy, fluoro or nitro, or thienyl; and η is 0 , 1, 2, or 3. 9 ♦ If applying for special A compound of formula I according to any one of items 2 to 4, wherein R 2 is Z · B- &lt; 5-(D) η Z is a Ο—, 〇 一 (Ci — C4) courtyard base one, one (Ci-C4) alkyl-101, S (0) 2-. 10. The compound of formula I according to any one of claims 1 to 4, wherein R 2 is -4-(please first Read the notes on the back and fill out this page) 本紙張尺度逋用中國國家梂準(CNS ) A4規格(21〇Χ:297公釐) 六、申請專利範圍 A8 B8 C8 D8 經濟部中央梂牟局貝工消費合作社印製 B 為 ( C 1 — C 4 ) 院 基 ♦ 鹵 — ( C 1 — C 4 ) 院 基 或 為 ( C 2 — C 4 ) 烯 基 或 ( C 2 — C 4 ) 炔 基 — ( C — C 2 ) 综 基 « 每 個 未 被 取 代 或 被 1 到 3 個 鹵 原 子 取 代 或 為 個 自 獨 立 地 被 ( C 1 — C 2 ) 院 基 » 鹵 素 — ( C 1 — C 2 ) 院 基 &gt; 鹵 素 &gt; 單 取 代 到 二 取 代 的 苯 基 i 或 為 R.5 Rt — (CHf 4 R9 r8 R 5 ) R a 和 R 9 個 自 獨 立 為 氫 &gt; ( C 1 — C 2 ) 基 t R 6 和 R 7 為 氬 或 ,素 0 1 1 • 如 申 請 專 利 範 圍 第 1 到 4 項 中 任 一 項 的 式 I 化 合 物 &gt; 其 中 R 2 為 4 — 位 置 被 — Ζ — Β 取 代 的 苯 基 0 1 2 • 如 申 請 專 利 範 圍 第 1 到 4 項 中 任 一 項 的 式 I 化 合 物 9 其 中 R 4 為 甲 基 或 苯 基 〇 1 3 • 如 申 請 專 利 範 圍 第 1 項 的 式 I 化 合 物 t 其 中 X 為 C Η ; Y 為 0 C Η 3 &gt; R 1 為 C Η 3 A 為 氧 R 2 為 4 — 甲 基 苯 基 或 4 — 烯 丙 氧 基 苯 基 或 4 — ( 3 — 二 氟 甲 基 — 苄 氧 基 ) 苯 基 或 4 — ( 2 2 一 二 氯 環 丙 基 甲 氧 基 ) 苯 基 和 R 3 為 C Η 3 0 1 4 • 如 申 請 專 利 範 圍 第 1 項 的 式 I 化 合 物 其 中 a ) X 為 氮 原 子 和 Y 為 0 C Η 3 或 N Η C Η 3 或 b ) X為C Η和 -5- 本紙張尺度適用中國國家梂準(CNS ) Α4规格(210Χ297公釐) -------,---.1.-衣------訂 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央梂準局男工消費合作社印製 々、申請專利範圍 Y 為◦ C Η 3 , 其中: Α為氧原子或NR#基; R!為氫,(Ci —C4 )烷基,環丙基,氰基或甲 基硫基; R2為氬;(C i - C 4 )烷基;環丙基;未被取代 的苯基或被個自獨立被鹵素,(C!— C4)烷基, (Ci—C*)烷氧基,(Ci— C2)鹵烷基,(Ci -C 2 )鹵烷氧基,(Ci - Cs )烯基氧基,(C3 -Cs )烯基氧基,(ct —C4 )次氧基二氧基單取代或 二取代的苯基;或噻吩基; R3為氫,(Ci 一 Cs )烷基,含1到5個鹵原子 的(C! — Ce )鹵烷基,(Ci - C 4 )烷氧基一 (C! 一 C 2 )烷基,(C 2 — C 4 )烯基,其係未被取代或被 1到3個鹵原子取代,(C2 — C4 )炔基,未被取代或 被1到2個鹵原子取代的環丙基甲基,氰基一 (C!—C4) 烷基;(Ci —C4 )烷氧基羰基一 (Ci — C2 )烷基 ,苯基—(Ci—C2)烷基,其係未被取代或被鹵素,_ (Ci - C 4 )鹵烷基,未被取代的苯基或被個自獨立被 (Ci— C4)烷基,(Ci—Cj)烷氧基,鹵素,含 1到3個鹵素原子的(Cz _Cz )鹵烷基,硝基單取代 或二取代的苯基,或未被取代的吡啶基或被含1到3個鹵 素原子的(C i — C 2 )鹵烷基或硝基取代的吡啶基; -6- 本紙張尺度逋用中國國家標準(CNS ) A4洗格(210X297公釐) (請先閱讀背面之注意事項再填寫本頁) 304860 ns8 D8 六、申請專利範圍 R4為(C! —C4 )烷基,苯基,或 R3和R4—起與其所鍵结的氮原子形成4一 (1 , 2 ,4 —三唑基),4 一嗎啉基或吖庚因基。 1 5 ·如申請專利範圍第1 4項的式ί化合物,其中 Α為氧, R i為甲基, R2為甲基;未被取代的苯基或獨立被鹵素,(C i 一 C4)烷基,(Ci— C4)烷氧基,(Ci—Cz) 鹵烷基,(Ci-Cz)-齒烷氧基,(C3-Ce)烯氧 基,(C3-C6)炔氧基,(Ci—C*)次烷基二氧 基單取代到二取代的苯基,或噻吩基;其和 R3 為(Ci — C6 )烷基。 1 6 ·如申請專利範圍第1 4項的式I化合物,其中 R3為氫;(C! — C4 )烷基;含1到3個鹵原子 的(Ci -C4 )鹵烷基;(Ci 一 C2 )烷氧基一( 經濟部中央標準局貝工消費合作社印製 I------·、一 衮------訂 (請先閱讀背面之注意事項再填寫本頁) C i &gt;一 C 2 )烷基;未被取代或被1到3個鹵原子取代的 丙:烯丙基;未被取代或被1到2個鹵原子取代的環 丙基甲基;氛基一(Cl — C2 )院基;(Cl —C2 ) 烷氧基羰基一 (Ci —c2 )烷基;未被取代或被鹵素, 含1到3個鹵原子取代的苯基;未被取代的苯基或被個自 獨立被鹵素,甲基,甲氧基,含1到3個鹵原子的鹵甲基 ,或硝基單取代或二取代的苯基;或未被取代的吡啶基或 被含1到3涸鹵原子的鹵甲基或硝基單取代吡啶基; -7 - 本紙張尺度逋用中國國家橾準(CNS ) A4洗格(210X297公釐) 經濟部中央揉準局貝工消費合作社印装 A8 B8 C8 D8 六、申請專利範圍 R4為甲基或苯基;或 R3和R4 —起與其所鍵结的氮原子形成4 — (1 , 2,4_三唑基),4_嗎啉基或吖庚因基。 1 7 ·如申請專利範圍第1 4項的式I化合物,其中 A為氧* R t為甲基, R2為甲基;未被取代的苯基或獨立被鹵素,甲基, 甲氧基,三氟甲基或三氟母基單取代到二取代的苯基; 和 - R 3為甲基。 1 8 ·如申請專利範圍第1 4的式I化合物,其中 A 為 N C Η 3 , R !為甲基, Rz為甲基;未被取代的苯基或獨立被鹵素,甲基, 甲氧基,三氟甲基或三氟甲氧基單取代到二取代的苯基; 和 R 3為甲基;未被取代的苯基或被個自獨立被鹵素, 甲基,甲氧基,含1到3個鹵原子的鹵甲基或硝基簞取代 或二取代的苯基;或未被取代的吡啶基或被含1到3涸鹵 原子的鹵甲基或硝基單取代的吡啶基。 1 9,如申請專利範圍第1項的式I化合物,其中 X為氮原子; Υ 為 0 R ! !; -8 _ 本紙張尺度適用中國國家揉準(CNS )八4規格(210X297公釐) --------' d 裝-- (請先閲讀背面之注意事項再填寫本頁) 訂 人 A8 B8 C8 ------ D8 、申請專利範圍 ν/ R 1 1為(Ci — C4 )烷基;其中 A ’ Ri ,R2和R3定義如如申請專利範圍第1項 0 2 0 ·如申請專利範圍第1項的式I化合物,其中 x為氮原子; (r12) Rl3 ; Rl 2和R! 3個自獨立為氫或(C! - C 4 )烷基 ’· #中A ’ R i ,R 2和R 3如申請專利範圍第1項所定 義。 _ 21 ·如申請專利範圍第20項的式I化合物,其中 Y 為 NH2 &gt; N (CH3)2 或 NHC2H5 ; A為氧原子; R 1和R 2為甲基; R3為氫;(C! _C4 )烷基;含1到3個鹵原子 的(C! ~c4 )鹵烷基;(Ct -Cz )烷氧基一( 經濟部中央橾準局負工消费合作社印策 -------¥ γ^------訂 (請先閲讀背面之注意事項再填寫本頁) C 1 一 C 2 )烷基;未被取代或被1到.3個鹵原子取代的 丙_基;烯丙基;未被取代或被丨到2個鹵原子取代的環 丙基甲基;氰基一(Ci 一(:2 )烷基;(Ct —C2 ) 烧氧基羰基—(Ci — C2 )烷基;未被取代或被鹵素, 含1到3個鹵原子,硝基取代的苯基;未被取代的苯基或 被涸自獨立被鹵素,甲基,甲氧基,含1到3個鹵原子的 鹵甲基,或硝基單取代或二取代的苯基;或未被取代的吡 啶基或被含1到3個鹵原子的鹵甲基或硝基lA代吡啶基 -9- 本紙張尺度逋用中國國家梯準(CNS ) A4規洛(210X297公釐) 經濟部中央標準局另工消費合作社印製 304860 含 8: D8 六、申請專利範圍 t 2 2 ·如申請專利範圍第2 1項的式I化合物,其中 R3為氫;(C, — C4 )烷基或含1到3個鹵原子 的(C i — C 4 )鹵烷基。 2 3 ·如申請專利範圍第1至4項中任一項的式I化合物 ,其中X = C雙鐽為E形式。 2 4 · —種製備如申請專利範圍第1項的式I化合物的方 法,其包括 (A )為了製得Y為N (-R i 2 ) R i 3之式I化合物, 使Y為0 R i :的式I化合物與Η N ( R 1 2 ) R : 3反應 ,該反應係於溶劑中在0到4 0 °C溫度下進行; (B)為了製得式I中之X,Y ,八和尺1 —R3如式I 所定義(其中R 3不為氫)的化合物,使下式肟 «2 HON^A 入D Π N R3 Ri 其中A和Ri —R3定義同上,與下式苄基衍生物反應 -10- 本紙張尺度適用中國國家橾準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再填寫本頁) 訂 A I申請專利範圍 〇The size of this paper adopts China National Standards (CNS) A4 specification (21〇Χ: 297 mm). Six, the scope of patent application A8 B8 C8 D8 The Ministry of Economic Affairs Central Bureau of Industry and Engineering Cooperative Printed B is (C 1 — C 4) Academy ♦ Halo — (C 1 — C 4) Academy is either (C 2 — C 4) alkenyl or (C 2 — C 4) alkynyl — (C — C 2) comprehensive base «each Unsubstituted or substituted with 1 to 3 halogen atoms or independently substituted by (C 1 — C 2) yard group »Halogen — (C 1 — C 2) yard group &gt; halogen &gt; monosubstituted to disubstituted The phenyl group i is R. 5 Rt — (CHf 4 R9 r8 R 5) R a and R 9 are independently hydrogen> (C 1 — C 2) The groups t R 6 and R 7 are argon or 0 1 1 • Compound of formula I as described in any one of items 1 to 4 of the patent application scope> wherein R 2 is a phenyl group substituted by — ZO — Β at the position 4 0 1 2 • As claimed in the patent application scope 1 to 4 Compound 9 of any one of formula I wherein R 4 is methyl or phenyl 〇1 3 • Compound I of formula I as in claim 1 of the patent application t wherein X is C Η; Y is 0 C Η 3 &gt; R 1 It is C Η 3 A is oxygen R 2 is 4-methylphenyl or 4-allyloxyphenyl or 4- (3-difluoromethyl-benzyloxy) phenyl or 4- (2 2 one two Chlorocyclopropylmethoxy) phenyl and R 3 are C Η 3 0 1 4 • Compounds of formula I as claimed in item 1 of the patent scope where a) X is a nitrogen atom and Y is 0 C Η 3 or N Η C Η 3 or b) X is C Η and -5- This paper size is applicable to China National Standards (CNS) Α4 specification (210Χ297mm) -------, ---. 1.-clothing --- --- Order (please read the precautions on the back before filling in this page) Printed by the Central Bureau of Economic Affairs of the Ministry of Economic Affairs, printed by the Male Workers ’Consumer Cooperative, and the scope of patent application Y is ◦ C Η 3, where: Α is oxygen atom or NR # Radical; R! Is hydrogen, (Ci —C4) alkane , Cyclopropyl, cyano or methylthio; R2 is argon; (C i-C 4) alkyl; cyclopropyl; unsubstituted phenyl or is independently halogenated, (C! — C4 ) Alkyl, (Ci—C *) alkoxy, (Ci—C2) haloalkyl, (Ci-C2) haloalkoxy, (Ci-Cs) alkenyloxy, (C3-Cs) alkene Yloxy, (ct —C4) hypooxydioxy mono- or di-substituted phenyl; or thienyl; R3 is hydrogen, (Ci-Cs) alkyl, containing 1 to 5 halogen atoms (C ! — Ce) haloalkyl, (Ci-C 4) alkoxy mono (C! — C 2) alkyl, (C 2 — C 4) alkenyl, which is unsubstituted or substituted by 1 to 3 halo Atomic substitution, (C2-C4) alkynyl, cyclopropylmethyl unsubstituted or substituted by 1 to 2 halogen atoms, cyano- (C! —C4) alkyl; (Ci —C4) alkoxy Carbonyl- (Ci-C2) alkyl, phenyl- (Ci-C2) alkyl, which is unsubstituted or halogenated, _ (Ci-C4) haloalkyl, unsubstituted phenyl or It is independently substituted by (Ci—C4) alkyl, (Ci—Cj) alkoxy, halogen, (Cz _Cz) haloalkyl containing 1 to 3 halogen atoms, or nitro Substituted phenyl, or unsubstituted pyridyl or pyridyl substituted with (C i — C 2) haloalkyl or nitro containing 1 to 3 halogen atoms; -6- This paper scale uses the country of China Standard (CNS) A4 wash grid (210X297mm) (Please read the precautions on the back before filling in this page) 304860 ns8 D8 6. The scope of patent application R4 is (C! —C4) alkyl, phenyl, or R3 and R4- and the nitrogen atom to which it is bonded form 4- (1, 2, 4-triazolyl), 4-morpholinyl or azepine. 1 5 · The compound of formula ί in item 14 of the patent application, wherein A is oxygen, R i is methyl, R 2 is methyl; unsubstituted phenyl or independently halogenated, (C i -C4) alkane Group, (Ci-C4) alkoxy, (Ci-Cz) haloalkyl, (Ci-Cz) -dentate alkoxy, (C3-Ce) alkenyloxy, (C3-C6) alkynyloxy, ( Ci-C *) monoalkyldioxy monosubstituted to disubstituted phenyl, or thienyl; and R3 is (Ci-C6) alkyl. 1 6 · The compound of formula I as claimed in item 14 of the patent scope, wherein R3 is hydrogen; (C! — C4) alkyl; (Ci -C4) haloalkyl containing 1 to 3 halogen atoms; (Ci one C2) Alkoxy 1 (printed by Peking Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs I ------ ·, Yiqu ------ order (please read the notes on the back before filling this page) C i &gt; one C 2) alkyl; unsubstituted or substituted with 1 to 3 halogen atoms propylene: allyl; unsubstituted or substituted with 1 to 2 halogen atoms cyclopropylmethyl; amido A (Cl — C2) alkynyl; (Cl — C2) alkoxycarbonyl one (Ci — c2) alkyl; unsubstituted or halogenated, phenyl containing 1 to 3 halogen atoms; unsubstituted Phenyl is either independently substituted by halogen, methyl, methoxy, halomethyl containing 1 to 3 halogen atoms, or nitro mono- or di-substituted phenyl; or unsubstituted pyridyl or by Halomethyl or nitro monosubstituted pyridyl groups containing 1 to 3 halo atoms; -7-This paper uses the Chinese National Standard (CNS) A4 wash grid (210X297 mm). Consumer Cooperative Printed A8 B8 C8 D8 Sixth, the scope of patent application R4 is methyl or phenyl; or R3 and R4 together with the nitrogen atom to which they are bonded to form 4- (1,2,4-triazolyl), 4-morpholinyl or Azepine. 1 7 · The compound of formula I as claimed in item 14 of the patent scope, wherein A is oxygen * R t is methyl, R2 is methyl; unsubstituted phenyl or independently halogenated, methyl, methoxy, The trifluoromethyl group or trifluoroparent group is mono- to di-substituted phenyl; and-R 3 is methyl. 1 8 · The compound of formula I as in claim 14 of the patent scope, wherein A is NC Η 3, R! Is methyl, Rz is methyl; unsubstituted phenyl or independently halogenated, methyl, methoxy , Trifluoromethyl or trifluoromethoxy mono-substituted to di-substituted phenyl; and R 3 is methyl; unsubstituted phenyl or independently halogenated, methyl, methoxy, containing 1 A phenyl group substituted or disubstituted with a halogenated methyl group or a nitrophosphate of up to 3 halogen atoms; or an unsubstituted pyridyl group or a pyridyl group mono-substituted with a halogenated methyl group or a nitro group containing 1 to 3 halogen atoms. 19, such as the compound of formula I in item 1 of the patent application, where X is a nitrogen atom; Υ is 0 R!!; -8 _ This paper size is applicable to China National Standard (CNS) 84 specifications (210X297 mm) -------- 'd outfit-(please read the precautions on the back before filling in this page) Subscriber A8 B8 C8 ------ D8, patent application scope ν / R 1 1 is (Ci -C4) alkyl; wherein A 'Ri, R2 and R3 are as defined in the patent application item 1 0 2 0. As in the patent application item 1 formula I compound, wherein x is a nitrogen atom; (r12) Rl3; Rl 2 and R! 3 are independently hydrogen or (C!-C 4) alkyl '· # 中 A' R i, R 2 and R 3 are as defined in item 1 of the patent application scope. _ 21 · The compound of formula I as claimed in item 20 of the patent scope, wherein Y is NH2> N (CH3) 2 or NHC2H5; A is an oxygen atom; R 1 and R 2 are methyl groups; R 3 is hydrogen; (C! _C4) alkyl; (C! ~ C4) haloalkyl containing 1 to 3 halogen atoms; (Ct -Cz) alkoxy one (Instigated by the Consumer Labor Cooperative of the Central Bureau of Economics of the Ministry of Economic Affairs ----- -¥ γ ^ ------ Order (please read the precautions on the back before filling in this page) C 1-C 2) alkyl; unsubstituted or substituted with 1 to .3 halogen atoms Group; allyl group; cyclopropylmethyl group which is unsubstituted or substituted by 1 to 2 halogen atoms; cyano- (Ci-(: 2) alkyl; — C2) alkyl; unsubstituted or halogen, containing 1 to 3 halogen atoms, nitro substituted phenyl; unsubstituted phenyl or benzyl is independently halogen, methyl, methoxy, containing Halomethyl with 1 to 3 halogen atoms, or phenyl mono- or di-substituted phenyl; or unsubstituted pyridyl or halogenated methyl with 1 to 3 halogen atoms or nitro 1A pyridyl -9- This paper scale adopts China National Standard (CNS) A4 regulation (210X297mm) Printed by the Central Standards Bureau of the Ministry of Economic Affairs, 304860, containing 8: D8. 6. Patent application scope t 2 2 · For example, the compound of formula I in item 21 of the patent application scope, where R3 is hydrogen; (C , — C4) alkyl or (C i — C 4) haloalkyl containing 1 to 3 halogen atoms. 2 3 • The compound of formula I as described in any of items 1 to 4 of the patent application, where X = C Shuangju is in the form of E. 2 4-A method for preparing the compound of formula I as claimed in item 1 of the patent application, which includes (A) in order to obtain the formula I where Y is N (-R i 2) R i 3 Compound, the compound of formula I with Y being 0 R i: reacts with H N (R 1 2) R: 3, the reaction is carried out in a solvent at a temperature of 0 to 40 ° C; (B) in order to obtain the formula X, Y, Ba and Chi 1 in I—R3 is a compound as defined in formula I (where R 3 is not hydrogen), so that the following formula oxime «2 HON ^ A is entered into D Π N R3 Ri where A and Ri — R3 The definition is the same as above, and it reacts with the benzyl derivative of the following formula -10- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) (please read the precautions on the back before filling in this page) Order A I Scope of patent application 〇 u A8 B8 C8 D8 III 其中X和Y定義同上,u為一離去基。反應係於惰性有機 稀釋劑中及鹼,有或無相轉移觸媒存在下,在Ot:到5 0亡 溫度進行。 (C)為了製備式I中之-A為氧,X,Y*Ri — R3如 式I所定義的化合物: 一下式肟 〇 HX Xu A8 B8 C8 D8 III where X and Y are as defined above, u is a leaving group. The reaction is carried out in an inert organic diluent and alkali, with or without phase transfer catalyst, at Ot: to 50 ° C. (C) In order to prepare the compound in which -A is oxygen, X, Y * Ri — R3 is as defined in the formula I: Y ΝY Ν ΟΗ Ν Ri IV -------' ,Ί裝------訂----- (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局貞工消费合作社印製 其中X,Y,Ri和尺2定義同上,與下式化合物反懕 U - R 3 V R3定義同式I ,卩定義同式I I I (R3既不是氫,也 不是苯基或吡陡基); 此反應為如(B )所述的親核性取代反應。 -1 1- 本紙張尺度逍用中國國家梂率(CNS) Μ規格(210X297公釐) 304S60 ABCD 六、申請專利範圍 (D)為了製備式I V中X,γ,Ri和R2如式I所定 義的化合物,使下式酮 h3c、 〇ΟΗ Ν Ri IV ------- ', Ί installed ------ ordered (please read the precautions on the back before filling out this page) Printed by the Zhengong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs Wherein X, Y, Ri and Ruler 2 are as defined above, and the compounds of the formula: U-R 3 V R3 are defined as Formula I, that is, as Formula III (R3 is neither hydrogen nor phenyl or pyridyl) ; This reaction is a nucleophilic substitution reaction as described in (B). -1 1- The size of the paper is used in the Chinese national frame rate (CNS) Μ specification (210X297 mm) 304S60 ABCD 6. Patent application scope (D) For the preparation of X, γ, Ri and R2 in formula IV as defined in formula I The compound of the formula ketone h3c, 〇 VI 其中X,Y,Ri和1?2同上所定義,與羥基胺或其鹽在 溶劑存在下於0°C到5 ου溫度下反應; (Ε)為了製備式I中A,X,丫和只! 一 R3如式I定 義,但R 3不為氫之化合物,使下式烯醇或肟 (請先閱讀背面之注意事項再填寫本頁) 裝 訂 經濟部中央標準局男工消費合作社印製 〇VI where X, Y, Ri and 1? 2 are as defined above, and react with hydroxylamine or its salt in the presence of a solvent at a temperature of 0 ° C to 5 ου; (Ε) In order to prepare A, X, Y and only! 1. R3 is as defined in Formula I, but R3 is not a hydrogen compound, so that the following formula is enol or oxime (please read the notes on the back before filling this page) Binding Printed by the Male Workers Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy 〇 A N— \闩3 VII 其中A,X,Y和R 1 — R 3如上定義,與甲基化試劑例 如甲基碘,二甲基硫酸鹽或二重氮甲烷反應,反應係於鹼 存在下於合適溶劑中進行。 25· —種製備式VII的方法 -1 2- 本紙張尺度逋用中a國家標準(CNS ) Α4規格(210X297公釐) Λ 36^860 Α8 Β8 C8 D8 申請專利範圍 〇 HOAN— \ Latch 3 VII where A, X, Y and R 1 — R 3 are as defined above, react with methylating reagents such as methyl iodide, dimethyl sulfate or diazomethane, the reaction is in the presence of alkali Carried out in a suitable solvent. 25 ·-A method for preparing formula VII -1 2- This paper uses the national standard (CNS) Α4 specification (210X297 mm) Λ 36 ^ 860 Α8 Β8 C8 D8 Patent application scope 〇 HO 〇/Ν&lt;γ/^Ν/ nr3 Ri VII 其中A,X,Y和Ri _R3定義同式I ,其包括 (A)製備式VI I中X為CH的化合物,其係使式VI I I的苯乙酸衍生物 〇〇 / Ν &lt; γ / ^ Ν / nr3 Ri VII where A, X, Y and Ri_R3 are defined as formula I, which includes (A) preparing a compound of formula VI I where X is CH, which is a benzene of formula VI II Acetic acid derivatives A vm (請先閲讀背面之注意事項再填寫本頁) 經濟部中央樣準局負工消費合作社印裂 其中A — R3定義同上,在鹼存在下與甲酸鹽反應 (B )製備式V I I中X為N的化合物,其係使式V I I I中其中A,丫和尺1 — Rs定義同上的苯基乙酸衍生物 在鹼存在下與亞硝酸或亞硝酸鹽反應; (C )製備式V I I中X為C Η的化合物,其係使式I X 的酮酯 -13- 本紙張尺度逋用中國國家標準(CNS &gt; Α4洗格(210X297公釐) 304860 A8 B8 C8 D8 申請專利範圍 〇A vm (Please read the precautions on the back before filling in this page) The Central Sample Bureau of the Ministry of Economic Affairs prints the negative labor consumption cooperative where A — R3 has the same definition as above and reacts with formate in the presence of alkali (B) in Formula VII X is a compound of N, which is a compound of formula VIII in which A, γ, and Chi 1 — Rs have the same definition as above, and the phenylacetic acid derivative reacts with nitrous acid or nitrite in the presence of a base; It is a compound of C Η, which uses the ketoester-13 of formula IX- This paper scale uses the Chinese National Standard (CNS &gt; Α4 wash grid (210X297 mm) 304860 A8 B8 C8 D8 to apply for patent scope. Υ NΥ N A Ny NRa Ri IX 經濟部中央標準局员工消費合作社印裝 其中A ,丫和尺! _R3定義同上,與甲氧基次甲基三苯 基磷烷反應; (D )製備式V I I中X為N的化合物,其像使式I X中 A,丫和}^1 _R3定義同上的萌酯與氧—甲基羥基胺或 其鹽反應。 - 2 6 · —種控制害蟲的組成物,其係包括如申請專利範圍 第1項的化合物作為活性成份,K及一種合適的載體。 2 7 ·如申請專利範圍第2 6項的組成物,其中害蟲為植 物致病微生物。 2 8 ·如申請專利範圍第2 7項的組成物,其中微生物為 徽菌。 29 ·如申請專利範圍第26項的組成物,其中害蟲為昆 蟲或恙蟲。 3 0 ·如申請專利範圍第1項的式I化合物在控制害蟲乏 應用。 3 1 · —種控制和預防害蟲的方法,其包括對害蟲或其居 住環境投與如申請專利範圍第1項的化合物。 32 ·如申請專利範圍第3 1項的方法,其害蟲為植物致 病性微生物。 -14 本紙張尺度適用中國國家梯準(CNS ) A4洗格(210X297公釐) (請先閱讀背面之注意事項再填寫本I) 304860 A8 B8 C8 D8 申請專利範圍3 3 ·如申請專利範圍第3 2項的方法,其中微生物為徽菌。34 ·如申請專利範圍第3 1項的方法,其中害蟲為昆蟲 或恙蟲。3 5 ·如申請專利範圍第3 1項的方法,其中種子被處理 0 36 · —種式V I I化合物 〇 HOA Ny NRa Ri IX Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economics Among them A, Ya and Chi! _R3 has the same definition as above, and reacts with methoxymethylenetriphenylphosphane; (D) Preparation of the compound of formula VII where X is N, which is like formula A, Y and} ^ 1 in formula IX _R3 has the same definition as Meng ester Reacts with oxygen-methylhydroxylamine or its salts. -2 6 ·-A pest control composition, which includes the compound as the first component of the scope of patent application as the active ingredient, K and a suitable carrier. 2 7 · For the composition of item 26 of the patent application scope, the pests are plant pathogenic microorganisms. 2 8 · For the composition according to item 27 of the patent application scope, the microorganisms are microbes. 29. For the composition according to item 26 of the patent application scope, the pests are insects or chiggers. 3 0 · The compound of formula I as the first item in the scope of patent application is used in the control of pest depletion. 3 1 · A method for controlling and preventing pests, which includes administering a compound such as item 1 of the scope of the patent application to the pests or their living environment. 32. If the method of claim 31 is applied, the pest is a plant pathogenic microorganism. -14 This paper scale is applicable to China National Standards (CNS) A4 Washing (210X297mm) (Please read the precautions on the back before filling in this I) 304860 A8 B8 C8 D8 Patent application scope 3 3 3 The method of item 2, wherein the microorganism is an emblem bacteria. 34. A method such as item 31 of the patent application scope, in which the pest is an insect or a tsutsugamushi. 3 5 · The method as claimed in item 3 1 of the patent application, wherein the seed is treated 0 36 ·-A compound of formula VI I 〇 HO A N R3 VII 其中A,X,丫和111 — R3定義如申請專利範圍第1項 37 · —種式VI I I化合物 (請先閱讀背面之注意事項再填寫本頁) 經濟部中夬標準局貝工消费合作社印裝AN R3 VII where A, X, YA and 111 — R3 is defined as in the scope of patent application item 1 37. — Compounds of formula VI II (please read the precautions on the back before filling out this page) Ministry of Economic Affairs Standards and Technology Bureau Printed by consumer cooperatives A ΥΙΠ 其中A,Υ和R: -R3定義如申請專利範圍第1項 -1 5- 本紙張尺度適用中國國家梂準(CNS ) A4规格(210X297公釐) 304860 8 888 ABCD 六、申請專利範圍 38 · —種式IX化合物 〇A ΥΙΠ where A, Υ and R: -R3 is defined as the first item of the patent application range -1 5- This paper size is applicable to China National Standards (CNS) A4 specifications (210X297 mm) 304860 8 888 ABCD VI. Patent application range 38 · a compound of formula IX A 3 R X T·* R 和 Υ A 中 其 項 1X 第 圍 範 πϋ 禾 專 請 如 義 定 3 R (請先閲讀背面之注意事項再填寫本頁) • V 衣-- 1 1 i 經濟部中央橾準局貝工消費合作社印裂 本紙浪尺度逍用中國國家揉準(CNS ) A4规格(210X297公釐)A 3 RXT · * R and Υ A of the terms 1X, the range of π, and the specific requirements, please specify Ru 3 R (please read the precautions on the back before filling this page) • V clothing-1 1 i Central Ministry of Economic Affairs The bureau's consumer cooperatives printed the cracked paper and used the Chinese standard (CNS) A4 specification (210X297mm)
TW83111584A 1994-01-05 1994-12-13 TW304860B (en)

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