An efficient and practical N-iodosuccinimide-promoted regioselective arylsulfenylation of imidazo[1,2-a]pyridines with disulfides has been developed to afford functionalized 3-sulfenylimidazo[1,2-a]pyridines heterocycles in moderate to good yields. Their structures were confirmed by IR, 1 H NMR, 13 C NMR and HRMS. Furthermore, this method has the advantages of mild reaction conditions, broad substrates scope and environmentally benign. Notably, the current methodology could also be conveniently applied to the synthesis of thioarylated naturally occurring biologically active frameworks.
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