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

  • Hu Wei ,
  • Long Yaqiu
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  • CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203

Received date: 2017-03-20

  Revised date: 2017-06-14

  Online published: 2017-07-07

Supported by

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

Abstract

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.

Cite this article

Hu Wei , Long Yaqiu . Cross-Dehydrogenative Coupling Reactions Applied in the Construction of Privileged Heterocycles[J]. Chinese Journal of Organic Chemistry, 2017 , 37(11) : 2850 -2858 . DOI: 10.6023/cjoc201703033

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