Invention Grant
- Patent Title: Formation of tetra-substituted enamides and stereoselective reduction thereof
- Patent Title (中): 四取代烯酰胺的形成及其立体选择性还原
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Application No.: US11629005Application Date: 2005-07-01
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Publication No.: US07629470B2Publication Date: 2009-12-08
- Inventor: Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
- Applicant: Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
- Applicant Address: US NJ Rahway
- Assignee: Merck & Co., Inc.
- Current Assignee: Merck & Co., Inc.
- Current Assignee Address: US NJ Rahway
- Agent Baerbel R. Brown; Catherine D. Fitch
- International Application: PCT/US2005/023514 WO 20050701
- International Announcement: WO2006/017045 WO 20060216
- Main IPC: C07D213/63
- IPC: C07D213/63

Abstract:
The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
Public/Granted literature
- US20090018340A1 Formation of Tetra-Substituted Enamides and Stereoselective Reduction Thereof Public/Granted day:2009-01-15
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