PdX2CuX2催化2-乙炔基苯胺衍生物环化反应：选择性合成2-取代-3-卤代-1H-吲哚化合物.pdfVIP

PdX /CuX -Catalyzed Annulation of 2 2 2-Ethynylbenzenamines: Selective Synthesis of 2-substituted-3-Halo-1H-indoles a，b a a b Tang Shi , Xie Yexiang , Li Jinheng *, Wang Naixing * a Key Laboratory of Chemical Biology Traditional Chinese Medicine Research (Ministry of Education), College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha, China (410081) b Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing, China (100101) E-mail：jhli@ Abstract A novel and effective protocol for the synthesis of 2-substituted-3-halo-1H-indoles by PdX / 2 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. 1. Introduction Indoles, in particular 3-halo-substituted ones, have attracted considerable efforts on their synthesis because this structural mot