Rhodium-Catalyzed C–H Functionalization Enabling Divergent Heterocycle Syntheses

Direct C–H bond functionalization represents a facile synthetic strategy that adheres to the principle of atom economy. Among a variety of metal catalysts, rhodium catalysts demonstrate distinctive advantages owing to their excellent reactivity. This account summarizes our recent advances in a series of rhodium-catalyzed C–H activation protocols, which enable diversified cyclization and cascade reactions with alkyne and alkene substrates, thereby efficiently constructing a broad range of heterocyclic scaffolds. These synthetic methodologies feature mild reaction conditions, high chemo- and regioselectivity, and remarkable step economy. Integrated with mechanistic investigations, several synthesized compounds exhibit promising antitumor potency, offering a new avenue for the discovery and development of bioactive molecules.