Synthesis of 2-Arylbenzothiazole and 2-Arylthiazole Derivatives via a Ru-Catalyzed <i>meta</i>-Selective C–H Nitration Reaction

Abstract

A Ru-catalyzed <i>meta</i>-selective C-H nitration of 2-arylbenzothiazoles and 2-arylthiazoles has been developed. A wide range of functional groups are tolerated, providing the <i>meta</i>-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.