Invention Grant
US08476437B2 Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
失效
制备（2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4] - 三唑并[4,3-a]吡嗪-7（8H） - 基 ] - （2,4,5-三氟苯基）丁-2-胺及其制备中的新杂质
![Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof](/docs/US/2013-07-02/US08476437B2/abs.jpg.600x600.jpg)
- Patent Title: Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
- Patent Title (中): 制备（2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4] - 三唑并[4,3-a]吡嗪-7（8H） - 基 ] - （2,4,5-三氟苯基）丁-2-胺及其制备中的新杂质
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Application No.: US13060388Application Date: 2009-08-26
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Publication No.: US08476437B2Publication Date: 2013-07-02
- Inventor: Himanshu Madhusudan Kothari , Mayank Ghanshyambhai Dave , Bipin Pandey , Bhavin Shriprasad Shukla
- Applicant: Himanshu Madhusudan Kothari , Mayank Ghanshyambhai Dave , Bipin Pandey , Bhavin Shriprasad Shukla
- Applicant Address: IN Ahmedabad
- Assignee: Cadila Healthcare Limited
- Current Assignee: Cadila Healthcare Limited
- Current Assignee Address: IN Ahmedabad
- Agency: IpHorgan Ltd.
- Priority: IN1798/MUM/2008 20080827; IN188/MUM/2009 20090202; IN785/MUM/2009 20090330
- International Application: PCT/IN2009/000470 WO 20090826
- International Announcement: WO2010/032264 WO 20100325
- Main IPC: C07D417/04
- IPC: C07D417/04
![Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof](/abs-image/US/2013/07/02/US08476437B2/abs.jpg.150x150.jpg)
Abstract:
The present invention relates to synthesis of β-amino acid derivatives of formula (I) and its salts of formula (Ia) by a novel process. The process comprises the reduction of a protected or unprotected prochiral β-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic β-amino compound is resolved to a pure stereoisomer of formula (I), specifically to (2R)-4-oxo-4-[3-Ctrifluoromethyl)-5,6-dihydrol[1,2,4]triazolo[4,3-alpyrazin-7(8H)-yl]-1-(2,4,4-trifluorophenyl)butan-2-amine. In an embodiment the invention disclosed polymorphic forms of formula (I), phosphate salt of formula (I) and also a Dibenzoyl-L-tartaric acid salt of formula (I).
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