Soluble polymer-supported synthesis of benzodiazepinones.
Soluble polymer-supported synthetic method provides a highly efficient route for the construction of biologically important 1,5-benzodiazepin-2-ones. A library of N-substituted benzodiazepinones can be readily assembled utilizing S(N)Ar reaction, reduction of nitro group and one-pot cyclization following N-alkylation as the key step in the synthesis. All reactions in the sequence were performed at room temperature to facilitate the generation of libraries in a parallel fashion. The crude products were obtained in 80-95% yield with 60-96% HPLC purity.
Wu
Cheng Yi
CY
Department of Chemistry, National Dong-Hwa University, Shou-Feng, 974, Hualien, Taiwan.
Sun
Chung Ming
CM
D001570:Benzodiazepinones / Q000138:chemical synthesis*; D020650:Combinatorial Chemistry Techniques; D011108:Polymers / Q000737:chemistry; D012995:Solubility
D001570:Benzodiazepinones; D011108:Polymers