First-Generation Route for CXCR7 Antagonist ACT-1004-1239 (1)

有机合成与工艺文献分享 2024-11-18 10:55

文章摘要

本文介绍了CXCR7拮抗剂ACT-1004-1239的首代合成路线，详细描述了从原料选择、反应条件优化到最终产物分离的整个过程。文章强调了在合成过程中遇到的挑战，如副产物的形成、溶剂选择以及产品过滤的困难，并通过实验优化解决了这些问题。最终，通过该路线成功合成了超过500克的API用于临床前活动，并在外部制造合作伙伴处生产了5.5千克的GMP材料用于Phase 1临床研究。

First-Generation Route for CXCR7 Antagonist ACT-1004-1239 (1)

查看文献： Development of a Scalable, Racemic First-Generation Route for CXCR7 Antagonist ACT-1004-1239 via cis-to-trans Epimerization and Subsequent Separation of Enantiomers
查看期刊：ACS Applied Electronic Materials

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