Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (11): 2850-2858.DOI: 10.6023/cjoc201703033 Previous Articles     Next Articles



胡玮, 龙亚秋   

  1. 中国科学院上海药物研究所 受体结构和功能重点实验室 上海 201203
  • 收稿日期:2017-03-20 修回日期:2017-06-14 发布日期:2017-07-07
  • 通讯作者: 龙亚秋
  • 基金资助:


Cross-Dehydrogenative Coupling Reactions Applied in the Construction of Privileged Heterocycles

Hu Wei, Long Yaqiu   

  1. CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203
  • Received:2017-03-20 Revised:2017-06-14 Published:2017-07-07
  • Contact: 10.6023/cjoc201703033
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81325020, 81761128022).

The reactions in which a new C-C bond is formed via a direct coupling of two C-H bonds are termed as cross dehydrogenative coupling (CDC). The coupling reactions would not need the pre-activation of the inert C-H bonds by any func-tional groups, featured with straightforwardness, atom-and step-economy and environmently benigness. Heterocycles are widely found in bioactive natural products and pharmaceuticals, designated as drug-like privileged scaffolds since they endowed diverse pharmacological effects. Preparation of these privileged structures by means of CDC confers distinctive advantages and enhances the discovery of lead compounds in medicinal chemistry. The application of CDC reactions in the synthesis of the heterocycles of pharmaceutical interest in recent years is summarized, focused on the construction of privileged scaffolds, such as indole, pyrrole, quinazoline, quinoxaline and the middle size and poly ring systems.

Key words: cross-dehydrogenative coupling, C-H functionalization, drug-like privileged scaffold