Synthesis of novel 2‐3‐methyl‐5‐[(E)‐2‐aryl‐1‐ethenyl]‐4‐isoxazolyl‐4,10a‐diaryl‐1,10a‐dihydro‐2H‐benzo[d]pyrazino[2,1‐b][1,3]oxazoles 5 were simply achieved by the reaction of 2‐[3‐methyl‐5‐[(E)‐2‐aryl‐1‐ethenyl]‐4‐isoxazolyl(2‐oxo‐2‐arylethyl)amino]‐1‐aryl‐1‐ethanones 3 with o‐aminophenol 4 in the presence of CAN catalyst. The intermediates, 2‐[3‐methyl‐5‐[(E)‐2‐aryl‐1‐ethenyl]‐4‐isoxazolyl(2‐oxo‐2‐arylethyl)amino]‐1‐aryl‐1‐ethanones 3, were prepared by the reaction of 4‐amino‐3‐methyl‐5‐styrylisoxazole 1, with phenacylbromides 2 in ethanol in the presence of K2CO3. The structures of the newly synthesized compounds 3a, 3b, 3c, 3d, 3e, 3f, 3g, 3h, 3i, 3j, 3k, 3l and 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j, 5k, 5l have been confirmed by analytical and spectral data.