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首页> 外文期刊>Angewandte Chemie >Formal Asymmetric Biocatalytic Reductive Animation
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Formal Asymmetric Biocatalytic Reductive Animation

机译:形式不对称生物催化还原胺化

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摘要

Asymmetric methods to prepare optically active a-chiral primary amines are highly demanded in asymmetric synthesis owing to the biological/pharmacological activity of many amines.Various techniques have been reported,such as asymmetric 1,2-addition to imines and asymmetric amination of a,a-disubstituted aldehydes,transformation of allylic alcohols into amines,(dynamic)kinetic resolution,and cyclic deracemization employing racemic amines as substrates.Asymmetric reductive amination of ketones has been investigated with transition-metal catalysts and organo-catalysts,as well as via sulfinyl imine intermediates.Although tremendous progress in organo/metal catalysis has been achieved for the asymmetric reductive amination of ketones to access alpha-chiral amines,improved protocols are still required that are simple,green,and economically viable and that lead to high enantiomeric excesses.
机译:由于许多胺的生物/药理活性,在不对称合成中对制备旋光性α-手性伯胺的不对称方法提出了很高的要求。已报道了多种技术,例如亚胺上不对称的1,2-加成和a,的不对称胺化, α-二取代醛,烯丙醇转化为胺,(动力学)动力学拆分和外消旋胺为底物的循环脱硫。已使用过渡金属催化剂和有机催化剂以及通过亚磺酰基研究了酮的不对称还原胺化尽管酮的不对称还原胺化反应在有机/金属催化方面取得了巨大进展,但仍需要改进的方案,该方案必须简单,绿色且经济可行,并导致对映体过量过多。

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