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Adagrasib’s Second-Generation Synthesis (3)

有机合成与工艺文献分享 2025-10-30 09:54
文章摘要
本文研究了Adagrasib第二代合成工艺中硫化物8的产率优化问题。背景显示该步骤在概念验证阶段产率仅为74%，主要因反应第二阶段中间体降解产生恶臭的2-丙硫醇和1,3-氧嗪酮杂质15。研究通过核磁分析证实首阶段形成环状半胺醛中间体，发现强碱条件导致开环副反应。实验表明添加MsCl可抑制杂质生成，进一步揭示体系中原位生成的HCl才是关键改进因素。最终筛选三氟甲磺酸替代强碱体系，不仅将产率提升至94%，还避免后处理步骤并将反应时间从18小时缩短至5小时，成功解决了放大生产中的搅拌难题。
Adagrasib’s Second-Generation Synthesis (3)
查看文献： Adagrasib’s Second-Generation Synthesis: Transitioning from Route Scouting to Optimization
查看期刊：Organic Process Research & Development
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