金催化2-炔基芳基叠氮与羧酸串联反应合成3-吲哚酯

Gold-Catalyzed Tandem Reactions of 2-Alkynyl Arylazides and Carboxylic Acids for the Synthesis of 1H-Indol-3-yl Esters

3-吲哚酯是一类十分重要的吲哚衍生物,存在于大量生物活性化合物或者天然产物中.通过金催化2-炔基芳基叠氮化合物产生金卡宾后被羧酸捕捉,有效合成了3-吲哚酯.作者在进行了大量的底物普适性测试后,提供了一种非常简单适用的3-吲哚酯合成方法.

1H-Indol-3-yl acetates are very important indole derivatives, which can be found in many bioactive compounds and natural products. In this work, 1H-indol-3-yl acetates were efficiently prepared via a-imino gold carbenes generated by gold-catalyzed reactions of 2-alkynyl arylazides. A very simple and general method for the synthesis of 1H-indol-3-yl acetates was provided after examining the substrates scope.