Zhang Zhenwei, Zhang Xiaoxue, Wang Hao, Xie Geyao, Zhou Yu
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences Hangzhou 310024 China
Drug Discovery & Development Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences Shanghai 201203 China.
RSC Adv. 2025 Jun 26;15(27):21872-21878. doi: 10.1039/d5ra01992c. eCollection 2025 Jun 23.
A catalytic system-controlled divergent reaction was reported to construct three distinct nitrogen-containing heterocycles from readily available starting materials a precise chemical bond activation and annulation cascade. Notably, this is the first capture of pyrazolidinones and propargyl alcohols to construct tetrahydropyrimidinones selective N-N bond activation and to generate previously unreported 3-acylindoles. This protocol demonstrates a broad substrate scope, moderate to good yields, and valuable transformations, laying a robust foundation for drug discovery applications.
据报道，一种催化体系控制的发散反应可从易得的起始原料构建三种不同的含氮杂环——一种精确的化学键活化和环化级联反应。值得注意的是，这是首次捕获吡唑烷酮和炔丙醇以构建四氢嘧啶酮——选择性N-N键活化并生成以前未报道的3-酰基吲哚。该方法展示了广泛的底物范围、中等至良好的产率以及有价值的转化，为药物发现应用奠定了坚实的基础。
