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Leveraging a High-Temperature Thermal Racemization

有机合成与工艺文献分享 2025-10-13 06:50
文章摘要
本文研究背景聚焦于有机合成中(P)-6阻转异构体的高对映体纯度需求，其异构化能垒高达42.3 kcal/mol。研究目的旨在开发高效的高温外消旋化工艺，以解决极性溶剂中分解严重的问题。通过实验发现，在315°C茴香醚中使用柱塞流反应器，仅需20分钟即可实现近完全外消旋且保持高纯度。结论表明该工艺可放大生产，通过碳酸钾萃取和结晶步骤从拆分废液中回收(P)-6，收率达90%，对映体过量值76%，为工业化应用提供了可行方案。
Leveraging a High-Temperature Thermal Racemization
查看文献： Axial Chirality in the Sotorasib Drug Substance, Part 2: Leveraging a High-Temperature Thermal Racemization to Recycle the Classical Resolution Waste Stream
查看期刊： Organic Process Research & Development
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