Cp*Rh(III)-Catalyzed Regioselective C(sp³)–H Electrophilic Trifluoromethylthiolation of 8‑Methylquinolines

Rh­(III)-catalyzed regioselective trifluoromethylthiolation of the unactivated C­(sp3)–H bond of 8-methylquinolines with bench-stable electrophilic trifluoromethylthiolating reagent via C­(sp3)–H activation is explored. Various substituted 8-methylquinolines provided the products in good yields with high regioselectivity. Current reaction conditions are also applicable for the late-stage functionalization of natural molecule santonin and caffeine-substituted 8-methylquinoline.