发明授权
US07824899B2 Preparation of enantiomerically enriched amines and amides by enzymatic resolution using a sulfonylacetic acid ester as acyl donor 失效
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

Preparation of enantiomerically enriched amines and amides by enzymatic resolution using a sulfonylacetic acid ester as acyl donor
摘要:
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.
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