Pd‐Catalyzed Denitrative C2‐Arylation of Oxazoles, Benzoxazoles, and Benzimidazoles with Nitroarenes

Abstract A step‐economic method for C2‐arylated azoles via Pd‐catalyzed denitrative arylation of nitroarenes and azoles is reported. This protocol employs synthetically upstream nitroarenes as arylating reagents and proceeds through the selective cleavage of the C−NO 2 and C−H bonds. Various nitroarenes and nitroheteroarenes were coupled with oxazoles, benzoxazoles, and methylbenzimidazoles, achieving yields of up to 95%. The method's utility is exemplified by its application in the synthesis of Flunoxaprofen. This strategy reduces synthetic steps and minimizes pollution, offering substantial cost‐effectiveness and environmental benefits. Furthermore, the relatively inert C−NO 2 bond in nitroarenes enables late‐stage functionalization or stepwise coupling reactions, providing a complementary method for C2‐arylation of azoles.