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Scalable Synthesis of C5aR1 Antagonist ACT-1014-6470 (3)

有机合成与工艺文献分享 2025-02-12 08:43
文章摘要
本文介绍了C5aR1拮抗剂ACT-1014-6470的规模化合成过程，重点讨论了酰胺还原步骤的挑战与解决方案。研究背景涉及药物合成中的关键步骤优化，研究目的是确保大规模生产的安全性和效率。通过实验，发现BH3·N,N-二乙基苯胺复合物（DEANB）在甲苯中于90-100°C条件下能实现完全转化和清洁产物形成。然而，过程中发现的安全风险促使研究团队在2.4公斤规模的放大实验中延长回流时间以确保安全。结论指出，尽管存在潜在的安全隐患，通过优化反应条件，成功实现了目标化合物的高效合成，且未检测到有害副产物。
Scalable Synthesis of C5aR1 Antagonist ACT-1014-6470 (3)
查看文献： Scalable Synthesis of C5aR1 Antagonist ACT-1014-6470 via N7-Selective Reductive Amination of an Unprotected Pyrazole Starting Material and Intramolecular Urea Formation with 1,1′-Carbonyl-di(1,2,4-triazol) (CDT)
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