Invention Grant
- Patent Title: Process for the preparation of endothelin receptor antagonists
- Patent Title (中): 制备内皮素受体拮抗剂的方法
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Application No.: US13127568Application Date: 2009-11-04
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Publication No.: US08404840B2Publication Date: 2013-03-26
- Inventor: Manne Satyanarayana Reddy , Chakilam Nagaraju , Achampeta Kodanda Ramprasad
- Applicant: Manne Satyanarayana Reddy , Chakilam Nagaraju , Achampeta Kodanda Ramprasad
- Applicant Address: IL Hyderabad, Andhra Pradesh
- Assignee: MSN Laboratories Limited
- Current Assignee: MSN Laboratories Limited
- Current Assignee Address: IL Hyderabad, Andhra Pradesh
- Agency: Hamilton, Brook, Smith & Reynolds, P.C.
- Priority: IN2712/CHE/2008 20081105; IN2713/CHE/2008 20081105; IN742/CHE/2009 20090331
- International Application: PCT/IN2009/000622 WO 20091104
- International Announcement: WO2010/070658 WO 20100624
- Main IPC: C07D239/02
- IPC: C07D239/02

Abstract:
The present invention relates to improved processes for the preparation of endolthelin receptor antagonists darusentan and ambrisentan, their salts and intermediates. Processes for the preparation of darusentan and ambrisentan comprise reacting benzophenone with a compound of Formula-3 to provide a compound of Formula-4, which on in-situ treatment with methanol and a suitable acid provides a compound of Formula-5; hydrolyzing the compound of Formula-5 to provide a compound of Formula-6; resolving the compound of Formula-6 to provide a compound of Formula-7; esterifying the compound of Formula-7 to provide a compound of Formula-8; reacting the compound of Formula-8 with a compound of Formula-9 to provide a compound of Formula-10; hydrolyzing the compound of Formula-10 to provide darusentan or ambrisentan; and purifiying darusentan or ambrisentan to provide darusentan or ambrisentan having purity greater than 99.00% by HPLC.
Public/Granted literature
- US20110263854A1 Improved Process For The Preparation Of Endothelin Receptor Antagonists Public/Granted day:2011-10-27
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