AR005119A1 - Procedimiento para la preparacion del compuesto intermediario n-acetil (l)-4-cianofenilalanina ac-(l)-phe(4-cn)-oh particularmente util en la preparacion de n-acetil-(l)-p-amidinofenilalanina-ciclohexilglicina-beta-(3-n-metilpiridinio) alanina y procedimietno para la prepracion del compuesto n-acetil-(l)-p-amidinofenilalanina-ciclohexilglicina-beta-(3-n-metilpiridinio) alanina - Google Patents
Procedimiento para la preparacion del compuesto intermediario n-acetil (l)-4-cianofenilalanina ac-(l)-phe(4-cn)-oh particularmente util en la preparacion de n-acetil-(l)-p-amidinofenilalanina-ciclohexilglicina-beta-(3-n-metilpiridinio) alanina y procedimietno para la prepracion del compuesto n-acetil-(l)-p-amidinofenilalanina-ciclohexilglicina-beta-(3-n-metilpiridinio) alaninaInfo
- Publication number
- AR005119A1 AR005119A1 ARP960105740A ARP960105740A AR005119A1 AR 005119 A1 AR005119 A1 AR 005119A1 AR P960105740 A ARP960105740 A AR P960105740A AR P960105740 A ARP960105740 A AR P960105740A AR 005119 A1 AR005119 A1 AR 005119A1
- Authority
- AR
- Argentina
- Prior art keywords
- alanine
- beta
- compound
- acetyl
- preparation
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P41/00—Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
- C12P41/003—Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions
- C12P41/005—Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions by esterification of carboxylic acid groups in the enantiomers or the inverse reaction
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P13/00—Preparation of nitrogen-containing organic compounds
- C12P13/04—Alpha- or beta- amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0815—Tripeptides with the first amino acid being basic
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P13/00—Preparation of nitrogen-containing organic compounds
- C12P13/02—Amides, e.g. chloramphenicol or polyamides; Imides or polyimides; Urethanes, i.e. compounds comprising N-C=O structural element or polyurethanes
Abstract
La presente invencion se refiere a un procedimiento para la preparacion de N-acetil-(l)-4-cianofenilalanina a partir del compuesto racemico ester etilicode N-acetil-(D,L)-cianofenilalanina comprendiendo las etapas de combinar dicho compuestoracemi co, una cantidad suficiente de una solucion acuosa, unacantidad suficiente de acetonitrilo, una cantidad suficiente de subtilisina para reaccionar con una cantidad sustancial del compuesto racemico para formarun medio de reaccion yajustar el med io de reaccion a un pH apropiado cuando se anade subtilisina y mantenimiento del pH apropiado mientras tiene lugar unareaccion para producir el compuesto deseado. Tambien se describe un procedimiento para la obtencion N-acetil-(L)-P-amido fenilalanina-ciclohexilglicina-Beta-(3-N-metilpiridinio)alanina que comprende las etapas de copular el intermediario N-acetil-(L)-4-cianofenilalanina con la amida de (L)-ciclohexilglicina-(L)-Beta-(3-piridil)-alanina yconversion, del grupo ciano de dicho compuesto copulado, en el grupo amidino y metilacion del nitrogeno delpiridilo para dar el compuesto deseado que es particularmente util en la inhibicion del factor Xa en la coagulacion de la sangre.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57556995A | 1995-12-20 | 1995-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR005119A1 true AR005119A1 (es) | 1999-04-14 |
Family
ID=24300839
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP960105740A AR005119A1 (es) | 1995-12-20 | 1996-12-18 | Procedimiento para la preparacion del compuesto intermediario n-acetil (l)-4-cianofenilalanina ac-(l)-phe(4-cn)-oh particularmente util en la preparacion de n-acetil-(l)-p-amidinofenilalanina-ciclohexilglicina-beta-(3-n-metilpiridinio) alanina y procedimietno para la prepracion del compuesto n-acetil-(l)-p-amidinofenilalanina-ciclohexilglicina-beta-(3-n-metilpiridinio) alanina |
Country Status (27)
| Country | Link |
|---|---|
| EP (1) | EP0868526B1 (es) |
| JP (1) | JP4044614B2 (es) |
| KR (1) | KR100438879B1 (es) |
| CN (1) | CN1087349C (es) |
| AR (1) | AR005119A1 (es) |
| AT (1) | ATE222293T1 (es) |
| AU (1) | AU717995B2 (es) |
| BR (1) | BR9612059A (es) |
| CA (1) | CA2241210C (es) |
| CZ (1) | CZ295362B6 (es) |
| DE (1) | DE69623038T2 (es) |
| DK (1) | DK0868526T3 (es) |
| EE (1) | EE03698B1 (es) |
| ES (1) | ES2179957T3 (es) |
| HK (1) | HK1017384A1 (es) |
| IL (1) | IL125003A (es) |
| MX (1) | MX9804997A (es) |
| NO (1) | NO319678B1 (es) |
| NZ (1) | NZ324159A (es) |
| PL (1) | PL185541B1 (es) |
| PT (1) | PT868526E (es) |
| RU (1) | RU2170764C2 (es) |
| SK (1) | SK281432B6 (es) |
| TR (1) | TR199801107T2 (es) |
| UA (1) | UA48993C2 (es) |
| WO (1) | WO1997022712A1 (es) |
| ZA (1) | ZA9610600B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9916732A (pt) * | 1999-01-02 | 2001-09-25 | Aventis Pharma Gmbh | Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa) |
| EP1016663A1 (en) * | 1999-01-02 | 2000-07-05 | Aventis Pharma Deutschland GmbH | Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity) |
| RU2250212C2 (ru) * | 2000-01-28 | 2005-04-20 | Авентис Фарма Дойчланд Гмбх | Способ получения ацетиламидиниофенилаланилциклогексилглицилпиридиниоаланинамидов |
| EP1127884A1 (en) * | 2000-02-26 | 2001-08-29 | Aventis Pharma Deutschland GmbH | Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them |
| PT1569912E (pt) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia |
| GB0306267D0 (en) * | 2003-03-19 | 2003-04-23 | Ineos Fluor Ltd | Process |
| JP2008260755A (ja) * | 2007-03-20 | 2008-10-30 | Sumitomo Chemical Co Ltd | Ｌ−ビフェニルアラニン化合物の塩の回収方法、およびそれを用いたビフェニルアラニンエステル化合物の回収方法 |
| CN106946724B (zh) * | 2017-04-07 | 2019-03-22 | 苏州汉德创宏生化科技有限公司 | 单胺基抑制剂类中间体2-乙酰氨基-2-苄基丙二酸单乙酯的合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4981799A (en) * | 1987-08-21 | 1991-01-01 | Takeda Chemical Industries, Ltd. | Acylamino acid racemase, production and use thereof |
| DE4115468A1 (de) * | 1991-05-11 | 1992-11-12 | Behringwerke Ag | Amidinophenylalaninderivate, verfahren zu deren herstellung, deren verwendung und diese enthaltende mittel als antikoagulantien |
| DE69213546T2 (de) * | 1991-05-13 | 1997-02-27 | Fujisawa Pharmaceutical Co | Neue Peptid-Verbindungen und Verfahren zur Herstellung davon |
| ATE262536T1 (de) * | 1994-04-26 | 2004-04-15 | Aventis Pharma Inc | Faktor xa inhibitoren |
-
1996
- 1996-11-25 CN CN96199198A patent/CN1087349C/zh not_active Expired - Fee Related
- 1996-11-25 CA CA002241210A patent/CA2241210C/en not_active Expired - Fee Related
- 1996-11-25 PL PL96327314A patent/PL185541B1/pl not_active IP Right Cessation
- 1996-11-25 BR BR9612059A patent/BR9612059A/pt not_active Application Discontinuation
- 1996-11-25 ES ES96942085T patent/ES2179957T3/es not_active Expired - Lifetime
- 1996-11-25 DE DE69623038T patent/DE69623038T2/de not_active Expired - Lifetime
- 1996-11-25 SK SK855-98A patent/SK281432B6/sk not_active IP Right Cessation
- 1996-11-25 JP JP52233697A patent/JP4044614B2/ja not_active Expired - Fee Related
- 1996-11-25 DK DK96942085T patent/DK0868526T3/da active
- 1996-11-25 KR KR10-1998-0704683A patent/KR100438879B1/ko not_active IP Right Cessation
- 1996-11-25 CZ CZ19981956A patent/CZ295362B6/cs not_active IP Right Cessation
- 1996-11-25 EP EP96942085A patent/EP0868526B1/en not_active Expired - Lifetime
- 1996-11-25 AU AU11251/97A patent/AU717995B2/en not_active Ceased
- 1996-11-25 IL IL12500396A patent/IL125003A/en not_active IP Right Cessation
- 1996-11-25 TR TR1998/01107T patent/TR199801107T2/xx unknown
- 1996-11-25 PT PT96942085T patent/PT868526E/pt unknown
- 1996-11-25 NZ NZ324159A patent/NZ324159A/xx not_active IP Right Cessation
- 1996-11-25 UA UA98062939A patent/UA48993C2/uk unknown
- 1996-11-25 RU RU98113301/04A patent/RU2170764C2/ru not_active IP Right Cessation
- 1996-11-25 EE EE9800188A patent/EE03698B1/xx not_active IP Right Cessation
- 1996-11-25 WO PCT/US1996/019005 patent/WO1997022712A1/en active IP Right Grant
- 1996-11-25 AT AT96942085T patent/ATE222293T1/de active
- 1996-12-17 ZA ZA9610600A patent/ZA9610600B/xx unknown
- 1996-12-18 AR ARP960105740A patent/AR005119A1/es active IP Right Grant
-
1998
- 1998-06-19 NO NO19982868A patent/NO319678B1/no not_active IP Right Cessation
- 1998-06-19 MX MX9804997A patent/MX9804997A/es not_active IP Right Cessation
-
1999
- 1999-05-25 HK HK99102351A patent/HK1017384A1/xx not_active IP Right Cessation
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