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高等学校化学研究 ›› 2015, Vol. 31 ›› Issue (4): 539-542.doi: 10.1007/s40242-015-5030-5

• Articles • 上一篇    下一篇

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
  • 收稿日期:2015-01-22 修回日期:2015-02-27 出版日期:2015-08-01 发布日期:2015-04-13
  • 通讯作者: WU Yong E-mail:wyong@scu.edu.cn
  • 基金资助:

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

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).

摘要:

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.

关键词: Negishi coupling, Almotriptan, 5-(Sulfamoylmethyl)indole

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