Synthesis of 2-Arylbenzothiazole and 2-Arylthiazole Derivatives via a Ru-Catalyzed meta-Selective C-H Nitration Reaction.

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.