BR9908207A - Processo para preparar um composto de n- [ ( (alifático ou aromático) carbonil] -2-aminoacetamida, e, isonitrila ligada à resina - Google Patents

Processo para preparar um composto de n- [ ( (alifático ou aromático) carbonil] -2-aminoacetamida, e, isonitrila ligada à resina

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Publication number
BR9908207A
BR9908207A BR9908207-1A BR9908207A BR9908207A BR 9908207 A BR9908207 A BR 9908207A BR 9908207 A BR9908207 A BR 9908207A BR 9908207 A BR9908207 A BR 9908207A
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BR
Brazil
Prior art keywords
compound
aliphatic
aromatic
replaced
optionally substituted
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Application number
BR9908207-1A
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English (en)
Inventor
Christopher Hulme
George C Morton
Joseph M Salvino
Richard F Labaudiniere
Helen J Mason
Matthew M Morissette
Liang Ma
Marie-Pierre Cherrier
Original Assignee
Aventis Pharm Prod Inc
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Application filed by Aventis Pharm Prod Inc filed Critical Aventis Pharm Prod Inc
Publication of BR9908207A publication Critical patent/BR9908207A/pt

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/14—Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/18—Oxygen or sulfur atoms
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    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Biochemistry (AREA)
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  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"PROCESSO PARA PREPARAR UM COMPOSTO DE N-[((ALIFáTICO OU AROMáTICO)CARBONIL]-2-AMINOACETAMIDA, E, ISONITRILA LIGADA à RESINA". A presente invenção diz respeito a um processo para preparar um composto de N-[((alifático ou aromático)carbonil]-2-aminoacetamida da fórmula (I) em que R~ a~ é (II) R~ aa~ é hidrogênio, alifático opcionalmente substituído ou aromático opcionalmente substituído; R~ b~ é hidrogênio, alifático opcionalmente substituído ou aromático opcionalmente substituído; R~ ca~ e R~ cb~ são independentemente hidrogênio, alifático opcionalmente substituído ou aromático opcionalmente substituído; R~ d~ é (III) e R~ da~ é alifático opcionalmente substituído ou aromático opcionalmente substituído; e R~ aa~ é substituído por uma amina protegida, primária ou secundária que na desproteção pode reagir com o carbono *ab ou *db, ou pelo menos um de R~ b~, R~ ca~ ou R~ cb~, onde cada um é substituído com pelo menos um ácido carboxílico ativado para formar um anel cíclico de 5 a 7 membros; ou R~ b~ é substituído com uma amina protegida, primária ou secundária que na desproteção pode reagir com o carbono *ab ou *db, ou pelo menos um de R~ aa~, R~ b~, R~ ca~, R~ cb~ ou R~ da~ onde cada um é substituído por pelo menos um ácido carboxílico ativado para formar um anel cíclico de 5 a 7 membros; ou R~ da~ e substituído por uma amina protegida, primária ou secundária que na desproteção pode reagir com pelo menos um de R~ ca~ ou R~ cb~ onde cada um é substituído por pelo menos um ácido carboxílico ativado para formar um anel cíclico de 5 a 7 membros, contanto que quando R~ aa~ for substituído por uma amina protegida, primária ou secundária que na desproteção pode reagir com R~ b~ substituído por pelo menos um ácido carboxílico ativado, então R~ aa~ é outro que não alifático substituído, que compreende reagir os quatro compostos seguintes: um composto de carbonila da fórmula (IV) um composto de amina da fórmula NH~ 2~R~ b~, um composto de isonitrila da fórmula NCR~ da~, e um composto ácido da fórmula R~ a~CO~ 2~H, para produzir o composto de N-[((alifático ou aromático)carbonil]-2-aminoacetamida, e o composto de N-[((alifático ou aromático)carbonil]-2-aminoacetamida. A invenção está também direcionada a um processo para ciclizar o composto de N-[(alifático ou aromático)carbonil]-2-aminoacetamida a um composto cíclico selecionado do grupo que consiste de um derivado de 1,4-benzodiazepina-2,5-diona, um derivado de dicetopiperazina, um derivado de cetopiperazina, um derivado de lactama, um derivado de 1,4-benzodiazapina e um derivado de diidroquinoxalinonas, e o composto ciclizado.
BR9908207-1A 1998-01-29 1999-01-29 Processo para preparar um composto de n- [ ( (alifático ou aromático) carbonil] -2-aminoacetamida, e, isonitrila ligada à resina BR9908207A (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US7300798P 1998-01-29 1998-01-29
US9840498P 1998-08-31 1998-08-31
US9870898P 1998-09-01 1998-09-01
US10105698P 1998-09-18 1998-09-18
PCT/US1999/001923 WO1999038844A1 (en) 1998-01-29 1999-01-29 Method for preparing an n-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound and a cyclyzed compound

Publications (1)

Publication Number Publication Date
BR9908207A true BR9908207A (pt) 2000-11-28

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BR9908207-1A BR9908207A (pt) 1998-01-29 1999-01-29 Processo para preparar um composto de n- [ ( (alifático ou aromático) carbonil] -2-aminoacetamida, e, isonitrila ligada à resina

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EP (1) EP1051397B1 (pt)
JP (1) JP2002501944A (pt)
KR (1) KR20010034469A (pt)
CN (1) CN1173946C (pt)
AP (1) AP1462A (pt)
AT (1) ATE419233T1 (pt)
AU (1) AU747987B2 (pt)
BG (1) BG65057B1 (pt)
BR (1) BR9908207A (pt)
CA (1) CA2318601A1 (pt)
DE (1) DE69940191D1 (pt)
EA (1) EA003061B1 (pt)
HU (1) HUP0101329A3 (pt)
IL (2) IL137571A0 (pt)
NO (1) NO324067B1 (pt)
OA (1) OA11475A (pt)
PL (1) PL342254A1 (pt)
SK (1) SK10642000A3 (pt)
WO (1) WO1999038844A1 (pt)

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