摘要/Abstract
报道了一种三氟甲磺酸催化下3-取代吲哚与(1H-2-吲哚基)二芳基甲醇的加成反应合成具有潜在生物活性2,3'-二吲哚衍生物的新方法.在最优化的反应条件下,以中等到高的产率得到了目标产物,且反应具有条件温和、操作简单、底物适用范围广等优点.同时,2-呋喃基二苯基甲醇也能够适用于反应当中,以较好的产率生成2-呋喃取代的吲哚衍生物.
关键词: 加成反应, 合成方法, 2,3'-二吲哚衍生物, 2-吲哚基二芳基甲醇, 三氟甲磺酸
A highly efficient TfOH-catalyzed addition of C3-substituted indole derivatives with (1H-indol-2-yl)diphenyl-methanols has been established, leading to the synthesis of a series of potentially bioactive 2,3'-bisindols in moderate to high yields (48%~89%) and with broad substrate scope under mild conditions. In addition, the furan-2-yldiphenylmethanol could also be applied in the reaction and afforded 2-(5-benzhydrylfuran-2-yl)-1H-indole in good yield.
Key words: addition reaction, synthetic method, 2,3'-bisindole derivatives, (1H-indol-2-yl)diphenylmethanol, TfOH
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