FIELD: pharmaceutical chemistry.
SUBSTANCE: invention relates to method for production of acetylamidiniophenylalanylcyclohexylglycilpypidinioalanin amides of formula I , wherein X anions are physiologically acceptable anions, and analogous thereof. Said compounds are effective inhibitors of fibrillation factor Xa and are useful, for example, in prevention of thrombosis. Claimed method includes coupling of 2-[2-acetylamino-3-(4-amidinophenyl)-propionylamino]-2-cyclohexylacetic acid, obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by assimetric hydration and converting of cyano group to amidine, or salt thereof with 3-(2-amino-2-carbamoylethyl)-1-methylpyridinic acid or salt thereof. Also are disclosed starting materials and intermediated used in this method, process for production the same and acetyl-(S)-4-amidiniophenylalanyl-(S)- cyclohexylglycil-(S)-(1-methyl-3-pypidinio)alanin amide in form of ditosylate.
EFFECT: simplified method; increased commercial availability of compounds with applicable anion.
14 cl, 16 ex
Title | Year | Author | Number |
---|---|---|---|
LIDINE-1-YL-ACETYLAMINO)-3-PHENYLPROPIONIC ACID ETHYL ESTER SALTS, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF | 1997 |
|
RU2174119C2 |
METHOD OF PRODUCING (1R,2R)-3-(3-DIMETHYLAMINO-1-ETHYL-2-METHYL-PROPYL)-PHENOL | 2007 |
|
RU2466124C2 |
HYDROGENATION OF IMINES | 2009 |
|
RU2476422C2 |
VERSIONS OF METHOD OF PRODUCING PYRIDINE-2-ETHERS OR PYRIDINE-2-THIOETHERS OR ACID-ADDITIVE SALTS THEREOF,OR PYRIDINE-N-OXIDES | 0 |
|
SU1417796A3 |
METHOD FOR PREPARING(-)-CIS-3-HYDROXY-1-METHYL-4-(2,4,6-TRIMETHOXYPHENYL)PIPERIDINE AND INTERMEDIATES COMPOUNDS | 1998 |
|
RU2265595C2 |
PRODUCTION OF COMPOUNDS AND COMPOSITIONS FOR SUPPRESSION OF SHP2 ACTIVITY | 2019 |
|
RU2797951C2 |
METHOD OF SYNTHESIS OF 3,7-DIALKYLXANTHINES | 1993 |
|
RU2114847C1 |
METHOD FOR PREPARATION OF ENANTIOMERICALLY AND DIASTEREOMERICALLY ENRICHED CYCLOBUTANE AMINES AND AMIDES | 2018 |
|
RU2793738C2 |
METHOD FOR PRODUCING FLUPIRTINE | 2010 |
|
RU2539298C2 |
SUBSTITUTED DERIVATIVES OF SULFONYLUREA OR THEIR SALTS USED IN AGRICULTURE AND HERBICIDE AGENT | 1992 |
|
RU2097380C1 |
Authors
Dates
2005-04-20—Published
2001-01-18—Filed