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...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.展开更多
A one pot protocol for the synthesis of dibenzodiazepinones was developed. The substituted ethyl 2- halobenzoates are cross-coupled with o-phenylenediamine utilizing a ligand-free, Cul catalyzed system, which spontane...A one pot protocol for the synthesis of dibenzodiazepinones was developed. The substituted ethyl 2- halobenzoates are cross-coupled with o-phenylenediamine utilizing a ligand-free, Cul catalyzed system, which spontaneously undergo an intramolecular N-acylation in ethylene glycol to give the corresponding products in high yields. This synthetic protocol provides a concise and efficient access to a wide variety of dibenzodiazepinone, including biologically active molecules.展开更多
基金supported by National Natural Science Foundation of China(No.81102322)
文摘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.
基金National Natural Science Foundation of China(No.81102322)the Global Alliance for TB Drug Development(TB alliance)for their financial supports
文摘A one pot protocol for the synthesis of dibenzodiazepinones was developed. The substituted ethyl 2- halobenzoates are cross-coupled with o-phenylenediamine utilizing a ligand-free, Cul catalyzed system, which spontaneously undergo an intramolecular N-acylation in ethylene glycol to give the corresponding products in high yields. This synthetic protocol provides a concise and efficient access to a wide variety of dibenzodiazepinone, including biologically active molecules.
