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Process for preparation of (2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro 1,2,4-triazolo4,3-apyrazin-7(8H)-yl-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
Process for preparation of (2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro 1,2,4-triazolo4,3-apyrazin-7(8H)-yl-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
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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