PdX2/CuX2-Catalyzed Annulation of 2-Ethynylbenzenamines: Selective Synthesis of 2-substituted-3-Halo-1H-indoles

Tang Shi; Xie Yexiang; Li Jinheng; Wang Naixing

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PdX2/CuX2-Catalyzed Annulation of 2-Ethynylbenzenamines: Selective Synthesis of 2-substituted-3-Halo-1H-indoles

Tang Shi 1,Xie Yexiang 2,Li Jinheng 2 * #,Wang Naixing 3

1.Hunan Normal University and Technical Institute of Physics and Chemistry, Chinese Academy of Sciences

2.Hunan Normal University

3.Technical Institute of Physics and Chemistry, Chinese Academy of Sciences

*Correspondence author

#Submitted by

Subject:

Funding: 教育部博士点基金（No.20060542007）

Opened online: 4 June 2007

Accepted by: none

Citation: Tang Shi,Xie Yexiang,Li Jinheng.PdX2/CuX2-Catalyzed Annulation of 2-Ethynylbenzenamines: Selective Synthesis of 2-substituted-3-Halo-1H-indoles[OL]. [ 4 June 2007] http://en.paper.edu.cn/en_releasepaper/content/13234

A novel and effective protocol for the synthesis of 2-substituted-3-halo-1H-indoles by PdX2/CuX2-catalyzed annulations of 2-ethynylbenzenamines has been developed. In the presence of PdX2 and CuX2, the annulation reactions of a variety of 2-ethynylbenzenamines were conducted in moderate to good yields. It is noteworthy that only N-acetyl protected 2-ethynylbenzenamines can undergo the reaction successfully.

Keywords:Palladium(II) halide, copper(II) halide, annulation, 2-ethynylbenzenamine, 2-substituted-3-halo-1H-indoles.

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