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Efficient Manufacturing Process for GDC-9545

有机合成与工艺文献分享 2024-12-25 07:20
文章摘要
本文介绍了GDC-9545的高效制造工艺，重点在于通过Pictet−Spengler反应构建关键中间体。文章探讨了多种合成tryptamine的方法，并最终选择了Wenker氮丙啶合成法，成功展示了从二甲酯24开始的100公斤规模的三步缩合工艺。研究还提出了替代工艺以解决原有工艺在规模化生产中的不足，特别是通过C−N偶联反应优化了氨基酸氮杂环丁烷中间体的构建。
Efficient Manufacturing Process for GDC-9545
查看文献： Efficient Manufacturing Process for the Selective Estrogen Receptor Degrader GDC-9545 (Giredestrant) via a Crystallization-Driven Diastereoselective Pictet–Spengler Condensation
查看期刊： Organic Process Research & Development
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