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,CuI 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
