Synthesis of trifluoromethylthiolated pyridinones through the copper-mediated trifluoromethylthiolation of iodopyridinones

An operationally simple method for the copper-mediated trifluoromethylthiolation of iodopyridinones employing (bpy) CuSCF3 (1; bpy = 2,2'-bipyridine) as a trifluoromethylthiolating reagent is presented. Various types of iodopyridinones are applicable and the trifluoromethylthiolated pyridinones are obtained in moderate to excellent yields. This method tolerates a variety of protecting groups on the nitrogen atom of pyridinones. In addition, scalability of the reaction is demonstrated.