PROCESS FOR THE PREPARATION OF 2-{4-[2-({[2-(4-CHLOROPHENYL)-1,3-THIAZOL-4-YL]METHYL}SULFANYL)-3,5-DICYANO-6-(PYRROLIDIN-1-YL)PYRIDIN-4-YL]PHENOXY}ETHYL-L-ALANYL-L-ALANINATE MONOHYDROCHLORIDE

• Main Authors: KEIL, BIRGIT, MAIS, FRANZ-JOSEF, OLENIK, BRITTA, BECKER, GUIDO, HEILMANN, WERNER
• Format: Patent
• Language: English; French
• Published: 01.12.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to a novel and improved process for the preparation of the compound 2-{4-[2-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)-pyridin-4-yl]-phenoxy}-ethyl-L-alanyl-L-alaninate monohydrochloride of formula (I), new precursors for their preparation, as well as to the production and use of the crystalline modification I of 2-{4-[2-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl]phenoxy}ethyl-L-alanyl-L-alaninate monohydrochloride of formula (I). La présente invention concerne un nouveau procédé amélioré de préparation du composé monohydrochlorure de 2-{4-[2-({[2-(4-chlorophényl)-1,3-thiazol-4-yl]méthyl}sulfanyl)-3,5-dicyan-6-(pyrrolidin-1-yl)pyridin-4-yl]-phénoxy}éthyl-L-alanyl-L-alaninate de formule (I), de nouveaux précurseurs pour sa préparation, ainsi que la préparation et l'utilisation de la modification cristalline I du monohydrochlorure de 2-{4-[2-({[2-(4-chlorophényl)-1,3-thiazol-4-yl]méthyl}sulfanyl)-3,5-dicyan-6-(pyrrolidin-1-yl)pyridin-4-yl]phénoxy}éthyl-L-alanyl-L-alaninate de formule (I).