Transition‐Metal‐Free Regioselective C−H Arylation of Heteroarenes

Abstract Regioselectively arylated heteroarenes are privileged scaffolds with remarkable biological and optoelectronic properties. Traditional arylation approaches based on the transition‐metal catalysis present various issues related to the cost of synthesis and environmental sustainability. The growing applications of arylheteroarenes in pharmaceuticals and cutting‐edge technologies have fuelled interest in the development of green and cost‐effective synthetic approaches. This article reports the recent progress in transition‐metal‐free strategies for the regioselective C−H arylation/heteroarylation of heteroarenes. C−H arylations of several five‐ and six‐membered, nitrogen, oxygen and sulphur containing heteroarenes using various arylation/heteroarylation reagents are comprehensively reviewed.