An efficient synthesis of substituted 1,4-diazepines is developed.The accessible intermediates have been obtained via Pd-catalyzed amination.The subsequent hydrogenation and intramolecular condensation sequences could be conducted successively in one pot without special operation.The mild and general strategy enables the synthesis of various substituted 1,4-diazepines in high yields. An efficient synthesis of substituted 1,4-diazepines is developed. The readily available intermediates have been obtained via Pd-catalyzedmination capable of sustaining in one pot without special operation. The mild and general strategy enables the synthesis of various substituted 1,4-diazepines in high yields.