3,5-disubstituted-1,2,4-oxadiazoles are undoubtedly one of the most important substructures present in many natural products,synthetic drugs and advanced functional materials.Traditional methods suffered from harsh reaction conditions(microwave radiation,high reaction temperature or some special catalysts) and the use of relatively unavailable starting materials.Hence,the development of a simple and efficient procedure for acquisition of 3,5-disubstituted-1,2,4-oxadiazoles from easily available starting materials under mild conditions continues to attract the interest of organic chemists due to their remarkable application value.Transition metal-catalyzed reactions have been attracted as a powerful tool for the formation of C-C,C-hetero and N-N bonds.Herein,we report a facile one-step synthesis of 3,5-disubstituted-1,2,4-oxadiazoles from amidines and methylarenes by copper-catalyzed cascade annulation,followed by Csp3-H oxidation of methylarenes under mild conditions.The reaction possesses an efficient oxidation-amination-cyclization tandem process and involves copper-catalyzed oxidative C-H bond acylation and C-N/C-O/N-O bond formations(Scheme 1).