Transition Metal‐Catalyzed Direct Functionalization of Carbazoles

Abstract Carbazoles are an important class of nitrogen‐containing heterocycles found in diverse natural products, bioactive molecules, and functional materials. Their broader applications have driven extensive research into their synthesis and functionalization. Among various approaches, transition metal‐catalyzed C−H activation has emerged as a powerful tool for direct functionalization, offering regioselectivity, efficiency, and sustainability. This review comprehensively summarizes advancements in transition metal‐catalyzed C−H functionalization of carbazoles. Various catalytic systems employing palladium, ruthenium, rhodium, nickel, cobalt, copper, and iron have enabled alkylation, alkenylation, acylation, arylation, alkynylation, and heteroatom incorporation in carbazoles. These methodologies enabled late‐stage diversification and have opened avenues for accessing structurally complex carbazole derivatives with tailored properties. The review aims to provide a comprehensive guide for researchers exploring carbazole functionalization via C−H activation, highlighting key mechanistic insights, scope, and emerging trends in this field.