Chemical Research in Chinese Universities ›› 2015, Vol. 31 ›› Issue (4): 539-542.doi: 10.1007/s40242-015-5030-5

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Synthesis of 5-(Sulfamoylmethyl)indoles by Mild Negishi Coupling and Their Application in Almotriptan

LI Xiaolong, QIU Rui, WAN Weili, CHENG Xu, HE Yi, HAI Li, WU Yong   

  1. Key Laboratory of Drug-Targeting and Drug-Delivery Systems of Ministry of Education, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, P. R. China
  • Received:2015-01-22 Revised:2015-02-27 Online:2015-08-01 Published:2015-04-13
  • Contact: WU Yong E-mail:wyong@scu.edu.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(Nos.81373259, 81102324).

Abstract:

A new synthetic route of almotriptan was described. The application of Negishi coupling reaction simplified the process and significantly improved the yield. The synthetic route was also expected to be general for the synthesis of other tryptamines like sumatriptan and avitriptan.

Key words: Negishi coupling, Almotriptan, 5-(Sulfamoylmethyl)indole