A Ru-catalyzed meta-selective C–H nitration of 2-arylbenzothiazoles and 2-arylthiazoles has been developed. A wide range of functional groups are tolerated, providing the meta-nitrated products in good to excellent yields using Cu­(NO3)2·3H2O as the nitro source. The nitration could be carried out on a gram scale and used for the synthesis of promising therapeutic leads for human African trypanosomiasis.

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A three-component cascade reaction of 1,3-enynes, anilines, and Togni-II reagent has been developed to give fully substituted trifluoromethyl pyrroles with high regioselectivity under mild conditions. The transformation proceeds through a Cu­(II)/Rh­(III)-promoted cascade aza-Michael addition/trifluoromethylation cyclization/oxidation reaction, affording trifluoromethyl pyrrole derivatives as primary products.

A simple and effective method for the synthesis of fully substituted 4-benzenesulfonyl isoxazoles through a copper­(II)-catalyzed three-component reaction of 2-nitro-1,3-enynes, amines, and sodium benzenesulfinate is described. The reaction proceeds smoothly under mild conditions and provides the benzenesulfonyl isoxazoles with high chemoselectivity.

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