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From Milligram to Kilogram Manufacture of AZD4573 (3)

有机合成与工艺文献分享 2024-09-19 07:27

文章摘要

本文讨论了AZD4573的制造过程，特别关注了从毫克到千克级别的生产工艺优化。文章提出了两种策略：酶催化的消旋酯的对映选择性水解（策略1）和酶催化的消旋氨基酯的对映选择性乙酰化（策略2）。通过引入新的构建模块15，避免了第一代合成中所需的脱保护/乙酰化策略。文章还探讨了构建模块A、B和C的组装方法，并选择了1H NMR监测作为分析工具。最终，通过筛选溶剂和碱，发现水性CH3CN与K2CO3的组合在反应中表现优异，被选为大规模生产16的首选方法。

From Milligram to Kilogram Manufacture of AZD4573 (3)

查看文献： From Milligram to Kilogram Manufacture of AZD4573: Making It Possible by Application of Enzyme-, Iridium-, and Palladium-Catalyzed Key Transformations
查看期刊： Organic Process Research & Development

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