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    • 9. 发明授权
    • Preparation of enantiomerically enriched amines and amides by enzymatic resolution using a sulfonylacetic acid ester as acyl donor
    • 使用磺酰基乙酸酯作为酰基供体通过酶拆分制备对映体富集的胺和酰胺
    • US07824899B2
    • 2010-11-02
    • US11766164
    • 2007-06-21
    • Harald GroegerOliver MayKai RossenKarlheinz Drauz
    • Harald GroegerOliver MayKai RossenKarlheinz Drauz
    • C12P41/00
    • C12P11/00C12P13/001C12P13/02C12P41/007
    • A process for the preparation of an enantiomerically enriched amine, is performed by a) cleaving a racemic mixture of a reaction product of i) a chiral amine and ii) an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; or b) reacting an amine with an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; and c) separating the enantiomerically enriched amide from the enantiomerically enriched amine, wherein the acyl donor is a sulphonylacetic acid ester. The process (1) leads to high enantioselectivities, and (2) high reactivities, (3) is based on an acyl donor accessible in a simple manner, (4) is suitable for a large number of very different substrates and/or (5) is suitable for carrying out at high substrate concentrations.
    • 通过a)在水解酶存在下,将i)手性胺和ii)酰基供体的反应产物的外消旋混合物切割,制备对映体富集的胺的方法,得到 对映异构体富集的酰胺和对映体富集的胺; 或b)在水解酶存在下使胺与酰基供体反应,得到对映体富集的酰胺和对映体富集的胺的混合物; 和c)从对映异构体富集的胺分离对映体富集的酰胺,其中所述酰基供体是磺酰基乙酸酯。 方法(1)导致高对映选择性,和(2)高反应性,(3)基于可以简单方式获得的酰基供体,(4)适用于大量非常不同的底物和/或(5 )适用于在高底物浓度下进行。