An efficient methodf or the oxidative cross-coupling of methylhetarenes with imidazoheterocycles by employing an eco-friendly iodine/DMSO reagent system has been developed.T his C(sp 2 )ÀHc arbonylation reactionp roceeds througha ni ns itu oxidation of am ethylhetarene into af ormylhetarene followed by an oxidative cross-coupling reaction with an imidazoheterocycle. This method has aw ide substrates cope and good functional group tolerance and enablest he constructiono falarge number of carbonylated imidazoheterocycles in very good yields.Scheme2.Oxidative couplings of 4-methylpyridine,b enzo[d]imidazo[2,1b]thiazole 9,a nd imidazopyridine 11. Scheme4.Putative reaction mechanism.Scheme3.Controle xperiments.

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