Abstract

We report a new facile synthesis procedure for the C-alkylation reaction of indole and indole derivative at 3-position with cyclic enol ethers in the presence of 2.5 mol% of I₂ under mild conditions. The optimum composition of the reaction mixture and catalyst were determined for maximum yield of C-alkylated indole derivative with molar ratio of indole derivative: cyclic enol ether was fixed at 1.0 equivalence: 1.5 equivalence with the presence of 2.5 mol% of I₂ in acetonitrile solvent and room temperature conditions. The results showed that under optimum conditions indole derivatives can be obtained good to excellent yields (80–92%) by the C-alkylation of indoles with cyclic enol ethers.

Graphic abstract

中文翻译：

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对吲哚3位C-烷基化新方法的研究

摘要

我们报道了在2.5mol％的I _2存在下在温和条件下3-位吲哚和吲哚衍生物与环状烯醇醚的C-烷基化反应的新的简便合成程序。确定反应混合物和催化剂的最佳组成，以C-烷基化的吲哚衍生物的最大收率与吲哚衍生物：环状烯醇醚的摩尔比固定为1.0当量：1.5当量，在乙腈中存在2.5 mol％的I ₂时溶剂和室温条件。结果表明，在最佳条件下，通过将吲哚与环状烯醇醚进行C-烷基化反应，可获得良好或优异的吲哚衍生物收率（80-92％）。

图形摘要