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Stereoselective Route for CXCR7 Antagonist ACT-1004-1239 (1)

有机合成与工艺文献分享 2025-02-03 14:11
文章摘要
本文介绍了一种立体选择性合成CXCR7拮抗剂ACT-1004-1239的路线。研究背景是传统的SMB分离方法时间长、成本高，因此需要开发一种更高效的立体选择性合成路线。研究目的是通过立体选择性还原手性胺衍生的烯胺，生产cis-3R,4S-异构体。研究过程中，团队探索了两种初始方法：酶动力学拆分和烯酰胺的对映选择性氢化。通过优化反应条件，团队成功开发了一种新的立体选择性还原序列，最终获得了高纯度的35-TFA（d.r. 98.2:1.8），并展示了该方法的简洁性和高效性。
Stereoselective Route for CXCR7 Antagonist ACT-1004-1239 (1)
查看文献： Development of a Scalable, Stereoselective Second-Generation Route for CXCR7 Antagonist ACT-1004-1239 via Chiral Enamine Reduction and a Novel Telescoped Sequence of Transesterification, cis-to-trans Epimerization, and Saponification
查看期刊：Organic Process Research & Development
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