公开(公告)号：US08247558B2

公开(公告)日：2012-08-21

申请号：US12439642

申请日：2007-09-04

Applicant: Parendn Dhirajlal Rathod ,  Satish Kumar Aryan ,  Ram Chander Aryan ,  Chandra Has Khanduri

Inventor： Parendn Dhirajlal Rathod ,  Satish Kumar Aryan ,  Ram Chander Aryan ,  Chandra Has Khanduri

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: The present invention provides a process for the preparation of clopidogrel and its pharmaceutically acceptable salts thereof comprises the resolving racemic methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate by the salt formation of methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate with excess levorotatory camphor-10-sulfonic acid to get a maximum yield of camphor sulphonate salt of methyl S-(+)-alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl) (2-chlorophenyl)-acetate and transforming the camphor sulphonate salt to clopidogrel or its pharmaceutically acceptable salts thereof.

Abstract translation: 本发明提供氯吡格雷及其药学上可接受的盐的制备方法，其包括拆分外消旋甲基α-5-（4,5,6,7-四氢[3,2-c]噻吩并吡啶基）（2-氯苯基） （4,5,6,7-四氢[3,2-c]噻吩并吡啶基）（2-氯苯基） - 乙酸甲酯与过量的左旋樟脑-10-磺酸形成盐，得到 甲基S - （+） - α-5-（4,5,6,7-四氢[3,2-c]噻吩并吡啶基）（2-氯苯基） - 乙酸酯的樟脑磺酸盐的最大产率，并转化樟脑磺酸盐 氯吡格雷或其药学上可接受的盐。