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手性叔胺-膦酰胺双功能催化剂催化华法林及其类似物的高对映选择性合成。

Highly enantioselective synthesis of warfarin and its analogs catalysed by primary amine-phosphinamide bifunctional catalysts.

机构信息

School of Chemical Engineering and Environment, Beijing Institute of Technology, Beijing 100081, People's Republic of China.

出版信息

Org Biomol Chem. 2012 Oct 28;10(40):8125-31. doi: 10.1039/c2ob26334c.

Abstract

An efficient enantioselective Michael addition of 4-hydroxycoumarin to α,β-unsaturated ketones catalysed by primary amine-phosphinamide bifunctional catalysts has been developed. This reaction afforded Warfarin and its analogs in moderate to excellent yields (up to 99%) and good to excellent enantioselectivities (up to 99% ee).

摘要

手性伯胺-膦酰胺双功能催化剂高效催化 4-羟基香豆素与α,β-不饱和酮的对映选择性迈克尔加成反应已被开发。该反应以中等到优异的收率(高达 99%)和良好到优异的对映选择性(高达 99%ee)得到了华法林及其类似物。

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