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Process Optimization of an RSV Drug Candidate (1)

有机合成与工艺文献分享 2024-12-12 08:31
文章摘要
本文讨论了针对RSV药物候选API 17的制造工艺优化。最初的生产路线提供了15公斤的API以支持早期临床开发，但由于异构杂质的竞争形成，吡唑并嘧啶核心5的产率较低。通过广泛的筛选，确定了三氟乙酸（TFA）作为减少异构杂质形成的首选添加剂，并在实验室规模测试了最佳条件。先前，化合物5的分离导致了化合物5（8%）和酸6（3-4%）的显著损失。通过减少异构杂质的水平，避免了中间体5的结晶，并采用了一种连续的反应步骤。
Process Optimization of an RSV Drug Candidate (1)
查看文献： High-Throughput Experimentation Enabling Rapid Process Optimization of an RSV Drug Candidate
查看期刊：Organic Process Research & Development
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