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Cost Driving Development of New Catalytic Asymmetric Routes (1)

有机合成与工艺文献分享 2025-07-02 08:05
文章摘要
本文介绍了辉瑞公司在制备nirmatrelvir过程中开发的新型催化不对称反应路线。研究背景是基于现有手性池方法的替代方案需求，旨在通过催化不对称反应制备片段3或其前体。研究目的集中在利用路易斯酸催化技术构建目标分子3的α-和γ-立体中心，并重点考察了迈克尔受体的N-取代基对反应活性的影响。研究结论表明，使用(Rp)-FesulPhos作为配体、1 mol%铜负载量以及2.5当量DIPEA时反应效果最佳，在5克规模反应中获得了67%的(S,S)-10·(−)-CSA分离收率。研究过程中还进行了高通量配体筛选和溶剂优化，证实了溶剂对反应的显著影响。
Cost Driving Development of New Catalytic Asymmetric Routes (1)
查看文献： Development of New Catalytic Asymmetric Routes toward a Cost-Driving Building Block of Nirmatrelvir
查看期刊：Organic Process Research & Development
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