Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (8): 2290-2307.DOI: 10.6023/cjoc202004024 Previous Articles     Next Articles

基于C(sp3)—H键断裂策略的杂环芳烃自由基烷基化反应进展

罗文坤a, 杨凯b, 尹标林a   

  1. a 华南理工大学化学与化工学院 广东省功能分子工程重点实验室 广州 510640;
    b 赣南医学院药学院 江西赣州 341000
  • 收稿日期:2020-04-14 修回日期:2020-05-09 出版日期:2020-08-25 发布日期:2020-05-20
  • 通讯作者: 杨凯, 尹标林 E-mail:kai_yangyang@126.com;blyin@scut.edu.cn
  • 基金资助:
    国家自然科学基金(No.21871094)及赣南医学院校级课题(No.YB201903)资助项目.

Recent Progress in Radical Alkylation of Heteroarenes Based on C(sp3)-H bond Cleavage Strategy

Luo Wenkuna, Yang Kaib, Yin Biaolina   

  1. a Key Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640;
    b College of Pharmacy, Gannan Medical University, Ganzhou, Jiangxi 341000
  • Received:2020-04-14 Revised:2020-05-09 Online:2020-08-25 Published:2020-05-20
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21871094) and the Scientific Research Project of Gannan Medical University (No. YB201903).

Heteroarenes are widely found in synthetic drugs and natural products and exhibit various biological activities. Among them, alkylated heteroarenes play a crucial role in the pharmaceutical industry, and have attracted great attention of synthetic chemists. C(sp3)-H bond cleavage strategy was widely used in radical alkylation of heteroarenes in organic synthesis and has been successfully applied in the total synthesis of natural products and pharmaceuticals due to its excellent atom economy. Based on the different precursor compounds (ethers, alcohols, amines, esters, amides and common alkanes), the research progress of radical alkylation of heteroarenes in a decade is summarized, and the related mechanism is also discussed.

Key words: C-H cleavage, heteroarene, radical, alkylation