Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (10): 2067-2085.DOI: 10.6023/cjoc201504013 Previous Articles     Next Articles



张英俊, 聂飚, 张霁   

  1. 广东东阳光集团药业研究院 东莞 523871
  • 收稿日期:2015-04-11 修回日期:2015-06-04 发布日期:2015-06-12
  • 通讯作者: 张霁
  • 基金资助:

    广东省引进创新科研团队计划(No. 201301Y0105381261)资助项目.

Progress in the Research of Copper Promoted C—H Functionalizations for the Synthesis of Fused Heterocycles Bearing Bridgehead Nitrogen

Zhang Yingjun, Nie Biao, Zhang Ji   

  1. HEC Pharm Group, HEC Research and Development Center, Dongguan 523871
  • Received:2015-04-11 Revised:2015-06-04 Published:2015-06-12
  • Supported by:

    Project supported by the Introduction of Innovative R&D Team Program of Guangdong Province (No. 201301Y0105381261).

The copper-catalyzed C—H activation, selective functionalization and the development of cyclization strategy for the synthesis of novel fused-heterocyclic (heterocycles with ring-junction nitrogen or bridgehead nitrogen) compounds are discussed. This class of novel bridgehead nitrogen heterocycles includes indolizine, pyrazolopyridine, benzimidazole and other polyheterocyclic compounds. The series including modern amination, oxidative coupling and Csp2—H, Csp—H, Csp3—H and N—H activation catalyzed by Cu(I) or Cu(II) salts makes this green synthesis a superior and practical method providing entry into complex heterocycles. Some reaction mechanisms have also been summarized.

Key words: copper-catalyzed, bridgehead nitrogen fused-heterocycles, oxidative coupling, C—H activation, N—H activation, cyclization, annulation