meta-Selective Substitution of Phenols with Indoles via One-Pot Oxidative Dearomatization-Michael Addition-Aromatization

Abstract

An oxidative coupling strategy involving hypervalent organoiodine-induced oxidative dearomatization of 4-substituted phenols, Brønsted acid catalyzed Michael addition with indoles, and aromatization has been developed. The one-pot reaction provides an efficient access to the meta-indole-substituted phenol derivatives.

Key words

aromatic substitution - biaryls - cross-coupling reaction - oxidation - regioselectivity

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