Hypervalent Iodine(III) Promoted Direct Synthesis of Imidazo[1,2‐a]pyrimidines

Abstract An efficient and mild synthesis of imidazo[1,2‐ a ]pyrimidine derivatives has been developed from readily available pyrimidyl arylamines or enamines through a hypervalent iodine‐promoted intramolecular C–H bond cycloamination reaction. This protocol allows for the facile construction of biologically active bicyclic imidazo[1,2‐ a ]pyrimidine skeletons as well as other imidazo[1,2‐ a ]‐type fused heterocycles.