Abstract

Iodine-mediated highly convenient strategy for the C-3 arylation of indoles with p-quinols is presented. The present work surpasses in forming a C–C bond at the meta-position of the phenols, which is traditionally challenging to functionalize. This protocol further leads the way to have ascendable, forthright access to phenol-assimilated heterocycles which have powerful applications both in synthetic and medicinal chemistry.

Graphic abstract

Iodine-mediated highly convenient and rapid protocol for C-3 arylation of indoles with p-quinols is presented. This methodology utilizes readily available indoles, furans and thiophene for Michael addition to p-quinols and subsequent aromatization to access phenol-assimilated heterocycles which have powerful applications both in synthetic and medicinal chemistry.

中文翻译：

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碘催化对苯二酚与吲哚的区域选择性C-3芳基化

摘要

提出了碘介导的吲哚与对苯二酚的C-3芳基化的高度方便的策略。目前的工作超出了在苯酚的间位形成C–C键的能力，这在功能上一直是一项挑战。该方案进一步引领了人们对苯酚类同化杂环的直接访问的途径，该类化合物在合成化学和药物化学中都有强大的应用。

图形摘要

提出了碘介导的对苯二酚与对苯二酚的C-3芳基化的高度方便和快速的方案。该方法利用容易获得的吲哚，呋喃和噻吩将迈克尔添加到对苯二酚中，随后进行芳构化，以得到在合成化学和药物化学中均具有强大应用的酚同化杂环。