吲哚的选择性酰化通常需要敏感和反应性的酰氯衍生物。这里,我们报告一个温和的,高效,功能组耐受性,以及使用硫酯作为稳定的酰基来源的吲哚的高度化学选择性N-酰化。已经以中等至良好的产率获得了一系列吲哚酰胺。此外,杂环,如咔唑,也可用作该反应中的亲核试剂。
The selective acylation of indoles often requires sensitive and reactive acyl chloride derivatives. Here, we report a mild, efficient, functional group tolerant, and highly chemoselective N-acylation of indoles using thioesters as a stable acyl source. A series of indoleamides have been obtained with moderate to good yields. In addition, heterocycles, such as carbazole, can also be used as nucleophiles in this reaction.