Invention Grant
US08314235B2 Process for preparing varenicline, varenicline intermediates, pharmaceutically acceptable salts thereof
失效
伐伦碱，伐伦碱中间体及其药学上可接受的盐的制备方法
- Patent Title: Process for preparing varenicline, varenicline intermediates, pharmaceutically acceptable salts thereof
- Patent Title (中): 伐伦碱，伐伦碱中间体及其药学上可接受的盐的制备方法
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Application No.: US13060755Application Date: 2009-08-31
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Publication No.: US08314235B2Publication Date: 2012-11-20
- Inventor: Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan
- Applicant: Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan
- Applicant Address: IS
- Assignee: Actavis Group PTC EHF
- Current Assignee: Actavis Group PTC EHF
- Current Assignee Address: IS
- Agency: Cantor Colburn LLP
- Priority: IN2133/CHE/2008 20080901
- International Application: PCT/IB2009/007081 WO 20090831
- International Announcement: WO2010/023561 WO 20100304
- Main IPC: C07D241/40
- IPC: C07D241/40
Abstract:
Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.
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