Benzodiazepines have powerful pharmacological effects and are a hot spot for medicinal chemistry and organic synthesis workers.In recent years,studies have found that 1,3-benzodiazepine derivatives are also bioactive and can also be used as clinical medicine.The synthetic method of con-structing 1,3-benzodiazepine derivatives via the 7-endo type nitroso-ene reaction.After converting the commercially available ortho-aminoacetophenone series compounds to hydroxamic acid,7-endo type ni-troso-ene reaction occurred in the CuC12/H2O2 system to produce 1,3-benzodiazepine derivatives.