有机小分子不对称催化Michael加成的研究进展

Progress in the Application of Organocatalysis to Asymmetric Michael Additions

有机小分子催化成为现在最热门的研究领域之一.不对称Michael加成反应是合成具有一个或多个手性中心合成砌块和药物中间体的重要方法.介绍了近3年来有机小分子伯胺衍生物、吡咯烷衍生物、(硫)脲、手性方酰胺和磷酸等在不对称催化Michael加成中的应用研究进展.对各种小分子结构和催化活性的关系、催化剂诱导活化机理以及各种催化体系在药物和关键中间体合成中的应用也进行详细的评述.

Organocatalysis has become one of the most intensively research fields. Asymmetric Michael addition is a key method for synthesis of versatile synthetic buildings and pharmaceutical intermediates, which include one or more stereo- chemical centers. The organocatalysts reported over the past three years for the asymmetric Michael addition are reviewed including primary amine, pyrrolidine based derivatives, （thio） urea, chiral squaramides and phosphoric acids. The relationship between structure of organocatalysts and their catalytic activities, catalytic reaction mechanism and the applications of these protocols for the preparation of drugs and bioactive intermediates are also introduced.