Herein, we introduce an unprecedented cascade reaction for the assembly of pyrrole-fused 1,5-benzodiazepine frameworks. These diverse privileged scaffolds were controllably constructed by intramolecular cyclization of β-enamino diketone, followed by annulation with o-phenylenediamine. The protocol features efficient one-pot cascade cyclization/annulation, performed under simple and mild reaction conditions. The products are obtained in a metal-free manner, in good to excellent yields (65–91%), and represent a fused heterocyclic scaffold that is not yet found in nature.

中文翻译：

---

β-烯氨基二酮和邻苯二胺的级联环化/环化：获得吡咯融合的 1,5-苯二氮卓类药物的策略


在此，我们介绍了一种前所未有的级联反应，用于吡咯熔融的 1,5-苯二氮卓类框架的组装。这些不同的特权支架是通过 β-烯氨基二酮的分子内环化，然后用邻苯二胺环化来控制构建的。该方案具有高效的一锅级联环化/环化，可在简单和温和的反应条件下进行。这些产品以无金属方式获得，产率从好到极高 （65-91%），代表了自然界中尚未发现的熔融杂环支架。