邻炔基苯胺的电化学环化合成3-碘吲哚

Electrochemical Annulations of o-Alkynylanilines for Synthesis of 3-Iodoindoles

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.

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.