An efficient synthesis of substituted 1,4-diazepines by a Pd catalyzed amination and sequential hydrogenation condensation

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.

Graphical abstractAn efficient synthesis of substituted 1,4-diazepines is developed. The mild and general strategy enables the construction of various substituted 1,4-diazepines in high yields.Figure optionsDownload full-size imageDownload as PowerPoint slide