In this work, we extend the one‐pot protocol to synthesize 1,2‐diazepines from commercially available and cheap starting materials. Capitalizing on isocyanate derivatives as activating agents, the photochemical skeletal enlargement occurs, while preserving key functional groups embedded in more than 30 substrates. We also demonstrated that isocyanates can be generated in situ exploiting the wealth of methods starting from bench stable resources. Compare to previous strategies, the use of these precursors prevents the presence of deleterious HCl traces in the system, thus enabling the synthesis of 1,2‐diazepines in high yields over up to 5 sequential steps.

中文翻译：

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用异氰酸酯改善吡啶类化合物向 1,2-二氮卓类化合物的光化学骨架增大


在这项工作中，我们扩展了一锅方案，从市售和廉价的起始材料合成 1,2-二氮卓类药物。利用异氰酸酯衍生物作为活化剂，发生光化学骨骼增大，同时保留嵌入 30 多种基材中的关键官能团。我们还证明，可以从工作台稳定的资源开始，利用丰富的方法原位生成异氰酸酯。与以前的策略相比，使用这些前体可以防止系统中存在有害的 HCl 痕量，从而能够在多达 5 个连续步骤中以高产率合成 1,2-二氮卓类药物。