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METHOD OF ENANTIOMERIC ENRICHMENT AND STEREOSELECTIVE SYNTHESIS OF CHIRAL AMINES

机译:手性胺的对映体富集和立体选择性合成方法

摘要

Amines in which the amino group is on a secondary carbon atom which is chirally substituted by R1 and R2 residuals, in which each of R1 and R2 is an alkyl or aryl group which is unsubstituted or substituted with an enzymatically non-inhibiting group and R1 is different from R2 in structure or chirality, said amines can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The transformation is carried out in the presence of an amino acceptor. Since the reaction is in an equilibrium, it can be reversed, whilst in this case it can be used for the stereoselective synthesis of one chiral form of an amine in the presence of depicted transaminase to a ketone in the presence of an amino donor.
机译:其中氨基在仲碳原子上的氨基被R1和R2残基手性取代的胺,其中R1和R2各自为未被取代或被酶促非抑制基团取代的烷基或芳基,R1为与R 2的结构或手性不同,所述胺可通过ω-氨基酸转氨酶的作用而对映体富集,所述ω-氨基酸转氨酶具有优先将两种手性形式之一转化为酮的性质。该转化在氨基受体的存在下进行。由于该反应处于平衡状态,因此可以逆转,而在这种情况下,它可以用于在氨基转移体存在的情况下,在所示的转氨酶存在下,将一种手性形式的胺立体选择性地合成为酮。

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