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通过支链醛的高对映选择性α-胺化反应有效地构建季立体中心。

Effective construction of quaternary stereocenters by highly enantioselective α-amination of branched aldehydes.

机构信息

Key Laboratory of Asymmetric Synthesis and Chirotechnology of Sichuan Province, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, 610041, China, PR.

出版信息

Org Biomol Chem. 2010 Oct 21;8(20):4524-6. doi: 10.1039/c0ob00406e. Epub 2010 Aug 23.

Abstract

A highly efficient enantioselective α-amination of branched aldehydes with azadicarboxylates promoted by chiral proline-derived amide thiourea bifunctional catalysts was developed for the first time, affording the adducts bearing quaternary stereogenic centers with excellent yields (up to 99%) and enantioselectivities (up to 97% ee).

摘要

首次发展了手性脯氨酸衍生酰胺硫脲双功能催化剂促进的氮杂二羧酸酯对支链醛的高效对映选择性α-胺化反应,得到了带有季立体中心的加合物,产率高达 99%(高达 97%ee)。

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