Cp*Co(III)‐catalyzed C–H functionalization of bioactive heterocyclic motifs

Abstract Cobalt catalysts are emerging as viable alternatives to precious transition metals such as palladium, rhodium, and ruthenium. Compared to rhodium(III) catalysts, cobalt(III) catalysts bearing pentamethylcyclopentadienyl ligands (Cp*) have demonstrated improved reactivity with enhanced chemo‐ or site‐selectivity. Notably, they exhibit robust and sustainable performance in the C–H functionalization of organic substrates, facilitating the synthesis of biologically active molecules. Moreover, this catalytic system is gaining considerable attention for late‐stage modifications owing to its cost‐effectiveness, sustainability, and lower toxicity. This review highlights recent advancements in Cp*Co(III)‐catalyzed C–H functionalization of biologically active scaffolds, including 6‐arylpurines, indoles, quinoline N ‐oxides, and heterocyclic drug molecules.