Organocatalytic Enantioselective Michael Addition of 4-Hydroxycoumarin to α,β-Unsaturated Ketones: A Simple Synthesis of Warfarin
Organocatalytic Enantioselective Michael Addition of 4-Hydroxycoumarin to α,β-Unsaturated Ketones: A Simple Synthesis of Warfarin
复制标题
DOI：
10.1002/ejoc.200900831
复制
发表时间：
2009-10-01
影响因子：
2.8
通讯作者：
Feng, Xiaoming
中科院分区：
文献类型：
--
作者：
Dong, Zhenhua;Wang, Lijia;Feng, Xiaoming
研制了一种c -2对称仲胺酰胺催化剂，用于4-羟基香豆素与α， β -不饱和酮的不对称Michael加成反应。在温和的条件下，以优异的收率（高达99%）和高的对映选择性（高达89% ee）获得了一系列重要的生物和药物活性化合物。此外，通过一次再结晶可以得到对映纯产物。（(C) Wiley-VCH Verlag GmbH & Co. KGaA，德国Weinheim 69451, 2009）
A type of C-2-symmetric secondary amine amide catalysts were developed for the asymmetric Michael addition of 4-hydroxycoumarin to alpha,beta-unsaturated ketones. A series of important biologically and pharmaceutically active compounds were obtained in excellent yields (up to 99%) with high enantioselectivities (up to 89 % ee) under mild conditions. In addition, enantiopure product could be obtained by a single recrystallization. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)