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双(三氟甲磺酰亚胺)钙催化1-取代氨基-2-芳基乙烯基1H -吲哚-1-羧酸酯的合成

张育莹a, 宋庆燕a, 李月容a, 郑怀基a,*, 魏邦国b   

  1. a西北农林科技大学化学与药学院 杨凌 712100;
    b复旦大学药学院 上海 200032
  • 收稿日期:2024-04-06 修回日期:2024-05-20
  • 基金资助:
    国家自然科学基金(No. 21772156)资助项目.

Ca(NTf2)2-catalyzed synthesis of 1-substituted amino 2-aryl vinyl 1H indole-1-carboxylates

Zhang yuyinga, Song qingyana, Li yueronga, Zheng huaijia,*, Wei, bangguob   

  1. aCollege of chemistry &Pharmacy, Northwest Agriculture & Forestry University, 3 Taicheng Road, Yangling 712100;
    bSchool of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203
  • Received:2024-04-06 Revised:2024-05-20
  • Contact: * E-mail: hjzheng@nwsuaf.edu.cn
  • Supported by:
    National Science Foundation of China (No. 21772156).

An efficient approach to access 1-substituted amino 2-aryl vinyl 1H indole-1-carboxylates 4a~o was achieved through Ca(NTf2)2-catalyzed addition process of ynamides 3 with tert-butyl 1-indolecarboxylate 2. After verification with 15 substrates, the yields of this method were stable between 52% and 87% and regioselectivities are excellent.

Key words: Calcium trifluoromethanesulfonimide, Ynamides, Indole, 1H indole-1-carboxylates, Regioselectivity