A simple, mild, and efficient oxidative copper-catalyzed regioselective trifluoromethylation of imidazo[1,5-a]-N-heteroarenes have been developed using Langlois , (NaSO 2 CF 3 ) reagent as CF 3 source. This method gives biologically relevant trifluorometh-ylated fused imidazoles in moderate to good yields with good functional group tolerance. The key features of the reaction are mild conditions, short reaction time, and room temperature reaction.

One‐pot sulfenylation/selenylation reaction have been developed to access 3‐sulfenyl/selenylimidazo[1,5‐a]quinolines from 2‐methylquinolines, aliphatic amines/amino acids and dichalcogenides. This developed method gives direct access to 3‐chalcogenylimidazo[1,5‐a]quinolines in moderate to good yields with good functional group tolerance from readily available starting materials. Moreover, this protocol can avoid the prior synthesis of fused imidazoles as starting materials for the synthesis of 3‐chalcogenylimidazo[1,5‐a]quinolines. Further, we have shown synthetic utility of 3‐sulfenylimidazo[1,5‐a]quinolines with m‐CPBA to afford corresponding sulfones in good to excellent yields.