Invention Grant
US09227965B2 Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV
有权
制备HCV大环蛋白酶抑制剂的方法和中间体
- Patent Title: Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV
- Patent Title (中): 制备HCV大环蛋白酶抑制剂的方法和中间体
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Application No.: US14345980Application Date: 2012-09-21
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Publication No.: US09227965B2Publication Date: 2016-01-05
- Inventor: Andras Horvath , Dominique Paul Michel Depré , Dominic John Ormerod
- Applicant: Janssen Pharmaceuticals, Inc.
- Applicant Address: US NJ Titusville
- Assignee: Janssen Pharmaceuticals, Inc.
- Current Assignee: Janssen Pharmaceuticals, Inc.
- Current Assignee Address: US NJ Titusville
- Agent Andrea Jo Kamage
- Priority: EP11182375 20110922
- International Application: PCT/EP2012/068593 WO 20120921
- International Announcement: WO2013/041655 WO 20130328
- Main IPC: C07D453/02
- IPC: C07D453/02 ; C07D453/04 ; C07D311/06 ; C07D417/04 ; C07C235/82

Abstract:
Disclosed is a process for the preparation of a cinchonidine salt of formula (IV) via an aqueous solution of a racemic 4-hydroxy-1,2-cyclopentanedicarboxylic acid, which is subjected to cyclization without removing water, by the addition of a water-miscible organic solvent to the aqueous solution and, again without removing water, adding cinchonidine to the aqueous-organic solvent solution so as to obtain the cinchonidine salt of the lactone acid. The cinchonidine salt is allowd to crystallize so as to obtain the enantiomerically purified crystalline lactone acid cinchonidine salt (IV). The enantiomerically pure salt is an intermediate in the synthesis of HCV inhibitor compound of formula (I).
Public/Granted literature
- US20140228574A1 Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV Public/Granted day:2014-08-14
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