Recent Advances in Transition Metal‐Catalyzed/Mediated CSCF3 Bond Formation Reaction

The trifluoromethylthiolated group (SCF 3 ) is characterized by its strong electron‐withdrawing ability, excellent lipophilicity, good stability, and bioavailability, making it highly relevant for applications in drug design and development. This review summarizes recent advances in CX (H, Cl, OTf, B(OH) 2 ) trifluoromethylthiolation reaction from 2014 to 2024. The discussion is organized into three major sections: 1) transition metal‐catalyzed CH trifluoromethylthiolation reactions facilitated by directing groups, 2) transition metal‐catalyzed trifluoromethylthiolation via cross‐coupling reactions, and 3) light‐assisted transition metal‐catalyzed trifluoromethylthiolation reactions. Additionally, this review examines the substrate scope, limitations, and partial mechanisms associated with these transformations.