【摘 要】
:
An efficient biocatalytic process has been developed to obtain optically pure(1S,4R)-N-(benzylcarbamoyl)-4-aminocyclopent-2-en-1-ol which can be used as the key
【机 构】
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State Key Laboratory of Chemical Resources Engineering, Beijing University of Chemical Technology,
【出 处】
:
Chinese Chemical Letters
论文部分内容阅读
An efficient biocatalytic process has been developed to obtain optically pure(1S,4R)-N-(benzylcarbamoyl)-4-aminocyclopent-2-en-1-ol which can be used as the key intermediate of ticagrelor. In this research, several N-(benzylcarbamoyl)-4-aminocyclopent-2-en-1-ol derivatives have been investigated in which Candida antarctica lipase B(CALB) was used to catalyze the asymmetric hydrolysis reaction. As expected, some of these substrates successfully gave(1S,4R)-N-(benzylcarbamoyl)-4-aminocyclopent-2-en-1-ol in >98% enantiomeric excess(ee) with conversion yields up to 45%.
An efficient biocatalytic process has been developed to obtain optically pure (1S, 4R) -N- (benzylcarbamoyl) -4-aminocyclopent-2-en-1-ol which can be used as the key intermediate of ticagrelor. In this research, several N- (benzylcarbamoyl) -4-aminocyclopent-2-en-1-ol derivatives have been investigated in which Candida antarctica lipase B (CALB) was used to catalyze the asymmetric hydrolysis reaction. As expected, some of these substrates were successfully given (1S , 4R) -N- (benzylcarbamoyl) -4-aminocyclopent-2-en-1 in> 98% enantiomeric excess (ee) with conversion yields up to 45%.
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