摘要/Abstract

吲哚及其衍生物是一类重要的杂环化合物, 也是多种天然产物和合成药物的骨架分子. 3-碘吲哚在其选择性功能化中充当着重要的中间体. 电化学氧化廉价易得的碘盐, 促使邻炔基苯胺分子内环化, 便捷地合成了一系列3-碘吲哚类化合物, 目标化合物可获得良好至优秀的产率. 该方法条件温和, 官能团适用范围广, 无需额外添加氧化剂和碱, 是一条操作简便、绿色可持续地合成3-碘吲哚类化合物的途径.
关键词: 电化学合成, 环化反应, 3-碘吲哚, 邻炔基苯胺
Indole, as one of the most important nitrogen-containing heterocyclic compound, is found widely in various natural products and synthetic drugs. 3-Iodoindoles play an important role as intermediate in the selective functionalization of indoles. 3-iodoindoles could be conveniently synthesized by electrochemical annulations of o-alkynylanilines with readily available iodide salt. This sustainable electrolysis strategy provides an efficient access to a series of 3-iodoindoles in good to excellent yields under external oxidant-free, base-free conditions and features broad functional group tolerance.
Key words: electrosynthesis, annulation, 3-iodoindoles, o-alkynylanilines


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