Abstract
Synthesis of N-benzylsclerotigenin was achieved in four steps. Initially, isatoic anhydride was allowed to react with benzylamine and chloroacetyl chloride, respectively. The generated dipeptide derivative was then cylized to [1,4]benzodiazepinedione. Acylation with o-nitrobenzoyl chloride furnished a labile [ 1,4] benzodiazepinedione derivative, which upon reduction afforded N-benzylsclerotigenin in high yield. This methodology can be adopted in combinatorial synthesis of N-substituted quinazolino[1,4]benzodiazepindione library for biological evaluation.