Research Progress of Rhodium(III)‐Catalyzed C(sp²)−H Bond Functionalization

Abstract Over the past decade, rhodium‐catalyzed C−H bond activation reactions have made significant progress and found broad applications in organic synthesis, biomedicine, and materials science. This is primarily attributed to their broad substrate scope, excellent functional group compatibility, and high reactivity. Currently, although considerable progress has been made, rhodium‐catalyzed C(sp 2 )−H functionalization still heavily relies on directing groups to achieve selectivity, which significantly diminishes the reaction's efficiency. Additionally, the challenge of selectively functionalizing remote (meta/para) C−H bonds further complicates research in this field. In this review, we primarily focus on the research progress in rhodium‐catalyzed C(sp 2 )−H functionalization from 2018 to 2024, categorizing reactions by type and providing a systematic overview of the mechanistic insights for each.