Abstract

Indole is an important heteroarene feature in many bioactive compounds, natural products, and functional materials. Hence, diversification of indoles by transition metal-catalyzed direct C-H activation has emerged as one of the most important topics in organic synthesis. Due to multiple C−H bonds with different reactive profiles in indoles, site selectivity is a long-standing challenge. The early developments focused primarily on C2-H and C3-H functionalization because of the inherent reactivity of the pyrrole ring. The recent focus on transition metal-catalyzed selective C−H functionalization on the benzenoid moiety at C4, C5, C6, and C7 positions provide direct access to diversely decorated indole compounds. This chapter describes contributions made in benzenoid ring C−H functionalization of indoles through transition metal catalysts.

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