An efficient, multicomponent and environmentally benign protocol has been developed for the synthesis of spiro-benzodiazepines through CC and CN bond formations in a single step. This one-pot protocol proceeds via three component reaction of o-phenylenediamines, tetronic acid and isatins by using mild and inexpensive catalyst like sulphamic acid in water. A variety of spiro-benzodiazepine derivatives has been synthesized in excellent yields by using this protocol in a shorter reaction time. All the synthesized compounds were evaluated for their cytotoxic potential on different human cancer cell lines and most of the compounds exhibited moderate to good cytotoxic activity, while some of them like 4f, 4h, 4i, 4j and 4q showed promising cytotoxicity with IC₅₀ values ranging between 1.14 and 1.69 μM.

已经开发出一种有效的，多组分的和环境友好的方案，用于在单个步骤中通过C C和C N键的形成来合成螺-苯并二氮杂ze 。通过使用温和且廉价的催化剂（如氨基磺酸）在水中使邻苯二胺，tetronic酸和isatins通过三组分反应进行这一一锅操作方案。通过使用该方案在较短的反应时间中，已以优异的产率合成了多种螺-苯并二氮杂卓衍生物。对所有合成的化合物在不同的人类癌细胞系中的细胞毒性潜力进行了评估，大多数化合物表现出中等至良好的细胞毒性活性，而其中一些化合物如4f，4h，图4i，4j和4q显示出有希望的细胞毒性，IC ₅₀值在1.14和1.69μM之间。