有机化学 ›› 2012, Vol. 32 ›› Issue (09): 1587-1604.DOI: 10.6023/cjoc201203009 上一篇    下一篇

综述与进展

有机小分子不对称催化Michael加成的研究进展

应安国, 武承林, 付永前, 任世斌, 梁华定   

  1. 台州学院医药化工学院 台州 318000
  • 收稿日期:2012-03-26 修回日期:2012-05-11 出版日期:2012-09-25 发布日期:2012-05-05
  • 通讯作者: 应安国 E-mail:agying@tzc.edu.cn
  • 基金资助:

    国家自然科学基金(No.21106090)、中国博士后基金面上(No.2012M511352)资助项目

Progress in the Application of Organocatalysis to Asymmetric Michael Additions

Ying Anguo, Wu Chenglin, Fu Yongqian, Ren Shibin, Liang Huading   

  1. School of Pharmaceutical and Chemical Engineering, Taizhou University, Taizhou 318000
  • Received:2012-03-26 Revised:2012-05-11 Online:2012-09-25 Published:2012-05-05
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.21106090) and the Postdoctoral Foundation of China (No.2012M511352)

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.

关键词: 不对称 Michael 加成, 有机催化, 对映选择性, 应用

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.

Key words: asymmetric Michael addition, organocatalysis, enantioselectivity, application