发明名称 |
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 |
摘要 |
The present invention relates to synthesis of beta-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 beta-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic beta-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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申请公布号 |
US8476437(B2) |
申请公布日期 |
2013.07.02 |
申请号 |
US200913060388 |
申请日期 |
2009.08.26 |
申请人 |
KOTHARI HIMANSHU MADHUSUDAN;DAVE MAYANK GHANSHYAMBHAI;PANDEY BIPIN;SHUKLA BHAVIN SHRIPRASAD;CADILA HEALTHCARE LIMITED |
发明人 |
KOTHARI HIMANSHU MADHUSUDAN;DAVE MAYANK GHANSHYAMBHAI;PANDEY BIPIN;SHUKLA BHAVIN SHRIPRASAD |
分类号 |
C07D417/04 |
主分类号 |
C07D417/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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