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Development and Scale-Up of KTX-005 (1)

有机合成与工艺文献分享 2025-06-03 08:32
文章摘要
本文主要介绍了药物KTX-005的开发和放大过程。背景方面，早期毫克级KTX-005的交付利用了Eli Lilly和Novo Nordisk报道的现有发现化学路线。研究目的是通过[3+2]-环加成反应构建所需的氮杂双环系统，并优化合成路线以提高产率和选择性。结论显示，虽然直接取代氯原子的尝试失败，但通过分步方法最终成功合成了(±)-KTX-005，并通过手性SFC分离得到两个对映异构体，总收率为6%。工艺优化中，溶剂从DMF改为DMA显著提高了目标产物的选择性（从70:30提高到93:7）。
Development and Scale-Up of KTX-005 (1)
查看文献： Development and Scale-Up of an Enabling Synthetic Route to KTX-005, a Muscarinic Acetylcholine Receptor Agonist for the Potential Treatment of Schizophrenia
查看期刊：Organic Process Research & Development
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