Process for the preparation of pleuromutilins

Details Process for the preparation of pleuromutilins Process for the preparation of pleuromutilins

C - Chemistry, Metallurgy

07

D

C07D 211/54 (2006.01) A61K 31/445 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2665347

A process for the preparation of 14-O-[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl) acetyl]mutilins of formula (I) feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O-[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.

L'invention concerne un procédé pour la préparation de 14-O-[(N-(3-méthyl-2-amino-butyryl-pipéridinyl)sulfanyl)acétyl]mutilines de formule (I), réalisable pour une production à grande échelle de produits de haute pureté, où l'atome de carbone sur le noyau pipéridine attaché à l'atome de soufre est soit dans la configuration (S), soit dans la configuration (R). L'invention concerne également une nouvelle forme cristalline de chlorhydrate de 14-O-[(N-3-méthyl-2-(R)-amino-butyryl-pipéridine-3(S)-yl)sulfanyl)acétyl]mutiline.

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