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Inherent Reactivity of API

有机合成与工艺文献分享 2025-09-21 06:54
文章摘要
背景：PF-06651600是一种高选择性口服JAK3抑制剂，其丙烯酰胺官能团具有固有迈克尔受体反应活性，在制备、纯化和储存过程中易产生加成杂质。研究目的：通过改进酰胺化工艺（使用3-氯丙酰氯替代丙烯酰氯）和开发稳定的单对甲苯磺酸盐结晶形式，解决杂质生成和原料药稳定性问题。结论：新工艺将杂质12的形成减少90%，获得的结晶盐符合固体选择标准并通过稳定性应力测试，中间体11经AMES试验确认为非基因毒性杂质。
Inherent Reactivity of API
查看文献： Process Development and Scale Up of a Selective JAK3 Covalent Inhibitor PF-06651600
查看期刊： Organic Process Research & Development
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