An efficient method for mono-phosphorylation of 2 （KRP203） using cbz-protection, dibenzylphosphoryl chloride and TMSI affording 2-P （KRP203-P） was developed. We applied the present method to the synthesis of KRP203 phosphate analogs which were difficult to produce through tradition procedures.
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.
Qing-Yang ZhangXiao-Jian WangYu-Lin TianJian-Guo QiChun Li Da-Li Yin
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.
