Integrated Ugi-Based Assembly of Functionally, Skeletally, and Stereochemically Diverse 1,4-Benzodiazepin-2-ones

A practical, integrated and versatile U-4CR-based assembly of 1,4-benzodiazepin-2-ones exhibiting functionally, skeletally, and stereochemically diverse substitution patterns is described. By virtue of its convergence, atom economy, and bond-forming efficiency, the methodology documented herein exemplifies the reconciliation of structural complexity and experimental simplicity in the context of medicinal chemistry projects.本研究报道了一种基于Ugi四组分反应（U-4CR）的实用、集成且通用的组装策略，可构建功能、骨架及立体化学取代模式均具多样性的1,4-苯并二氮杂䓬-2-酮类化合物。该方法凭借其收敛性、原子经济性与成键效率，在药物化学研究项目中，彰显了结构复杂性与实验操作简便性的有机统一。