Sulfonylation of quinoline N-oxides with aryl sulfonyl chlorides via copper-catalyzed C-H bonds activation.

An efficient and concise one-pot protocol to synthesize sulfonylated quinoline N-oxides via copper-catalyzed C-H bond activation has been developed. Commercially available and less expensive aryl sulfonyl chlorides were used as the sulfonylation reagents. Various 2-aryl sulfonyl quinolines were obtained in up to 91% yields in chemo- and regioselective manners.