The production of effective drugs has continuously been a challenging process for researchers due to the occurrence of resistive diseases. Drugs derived from natural product-based compounds as an active scaffold have gained interest in drug development due to a wide range of biological properties. Benzoheterodiazepines, a natural product derivative of bicyclic chalcones have been widely reported with various therapeutic potentials. This review discusses current synthetic methods in the preparation of benzoheterodiazepine derivatives (i.e., homocyclic benzoheterodiazepine, heterocyclic benzoheterodiazepine, bis-benzoheterodiazepine, and fused benzoheterodiazepine) via two-pot and one-pot synthetic routes. Several reaction protocols following both synthetic routes have been developed for efficient and higher yields that offer access to different functionalization of benzoheterodiazepines are comprehensively described. This review is important in the heterocyclic chemistry of benzoheterodiazepines and pharmacological industries in drug development processes.

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查尔酮衍生的苯并杂二氮卓类药物应用：两锅和一锅合成方法

由于耐药性疾病的发生，有效药物的生产一直是研究人员面临的挑战。由于具有广泛的生物学特性，从基于天然产物的化合物中提取的药物作为活性支架在药物开发中引起了人们的兴趣。苯并杂二氮卓类是双环查耳酮的天然产物衍生物，已被广泛报道，具有多种治疗潜力。本综述讨论了目前制备苯并杂二氮杂卓衍生物（即同环苯并杂二氮杂、杂环苯并杂二氮杂-苯并杂二氮杂和稠合苯并杂二氮杂）通过两锅和一锅合成路线。已经开发了几种遵循这两种合成路线的反应方案，以实现高效和更高的产率，全面描述了苯并杂二氮卓的不同功能化。这篇综述对苯并杂二氮卓类的杂环化学和药物开发过程中的药理学工业很重要。