Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (5): 1029-1034.DOI: 10.6023/cjoc201712010 Previous Articles     Next Articles



薛红, 董玉, 冯磊, 李海波, 李津, 张志伟   

  1. 河北科技大学化学与制药工程学院 石家庄 050018
  • 收稿日期:2017-12-06 修回日期:2018-01-06 发布日期:2018-01-18
  • 通讯作者: 张志伟,
  • 基金资助:


Research Progress in the Synthesis of 3-Indolecarboxylates

Xue Hong, Dong Yu, Feng Lei, Li Haibo, Li Jin, Zhang Zhiwei   

  1. College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018
  • Received:2017-12-06 Revised:2018-01-06 Published:2018-01-18
  • Contact: 10.6023/cjoc201712010
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21302039) and the Natural Science Foundation of Hebei Province (No. B2016208124).

Indole derivatives have been considered as “privileged scaffolds” in drug discovery since they are capable of binding many receptors with high affinity. 3-Indolecarboxylates are widespread structure motifs in many natural products and drug molecules, such as arbidol, tropisetron, PD 0298029, and grandilodine A, etc. Consequently, synthetic studies toward 3-indolecarboxylates have been reported in recent years. Elegant cyclization strategies have been developed via transition-metal catalyzed or transition-metal-free reactions, and direct functionalization at C-3 position for synthesis of ester functional groups was also extremely attractive. Based on our studies toward synthesis of 3-indolecarboxylates, the recent developments of synthesis of 3-indolecarboxylates by different synthetic methods in view of the types of substrates are reviewed.

Key words: 3-indolecarboxylate, metal-catalyzed cyclization, C—H functionalization, transition metal-free reaction, recent development