Process for the preparation of s-(+)-clopidogrel by optical...

Details Process for the preparation of s-(+)-clopidogrel by optical... Process for the preparation of s-(+)-clopidogrel by optical...

C - Chemistry, Metallurgy

07

D

C07D 495/04 (2006.01) A61P 7/02 (2006.01) A61P 9/10 (2006.01) C07D 498/02 (2006.01) C07D 513/08 (2006.01)

Patent

CA 2635255

The present invention relates to a process for the preparation of S-(+)- clopidogrel by an optical resolution and, more particularly, to a process for the preparation of S-(+)-clopidogrel represented by the following formula 1 with high optical purity by converting a clopidogrel racemic carboxylic acid into a diastereomeric salt using a (+)-cinchonine for optical resolution, extracting an S-(+)-clopidogrel carboxylic acid from the diastereomeric salt using a suitable solvent under an acidic condition and then reacting the S-(+)- clopidogrel carboxylic acid with methanol.

La présente invention concerne un procédé destiné à la préparation de S-(+)-clopidogrel par résolution optique et, plus précisément, un procédé destiné à la préparation de S-(+)-clopidogrel représenté par la formule générale (1), de grande pureté optique. Ce procédé consiste à convertir un acide carboxylique racémique de clopidogrel en sel diastéréomérique à l'aide d'une (+)-cinchonine pour la résolution optique, à extraire un acide carboxylique de S-(+)-clopidogrel à partir du sel diastéréomérique à l'aide d'un solvant adapté dans des conditions acides, puis à faire réagir l'acide carboxylique de S-(+)-clopidogrel avec du méthanol.

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