METHOD OF PREPARING CLOPIDOGREL AND INTERMEDIATES USED THEREIN

摘要

A method for preparing clopidogrel is provided to obtain optically pure clopidogrel with high yield through a simple process, which is used for treating peripheral arterial diseases and ischemic heart diseases. The method comprises the steps of: (a) reacting a (Œ)-alpha-(2-chlorophenyl)-6,7-dihydro-4H-thieno[3,2-c]pyridine-5-acetic acid represented by the formula(2) with an optically active amine derivative to crystallize a salt of a partial stereoisomer thereof represented by the formula(4) and then isolating the optically active derivative from the salt to obtain (S)-(+)-alpha-(2chlorophenyl)-6,7-dihydro-4H-thieno[3,2-c]pyridine-5-acetic acid represented by the formula(3) or an acid-addition salt thereof; and (b) methyl-esterifying the compound represented by the formula(3) or the acid-addition salt thereof to obtain a clopidogrel represented by the formula(1).