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Early Process Development of an LPAR1 Antagonist

有机合成与工艺文献分享 2025-02-24 07:11
文章摘要
本文介绍了LPAR1拮抗剂GS-2278的早期工艺开发过程，该药物用于治疗特发性肺纤维化。研究背景涉及通过交叉偶联生成三唑核心的替代路线，但Negishi偶联因规模依赖性限制了产量。研究目的是优化工艺以提高产量和安全性，通过评估不同条件，发现双缩合产物为主要问题。结论指出，通过添加LiCl解决了金属化过程中的凝胶问题，并优化了2-MeTHF中的连续工艺，最终实现了更稳健的生产过程。
Early Process Development of an LPAR1 Antagonist
查看文献： Early Process Development of an LPAR1 Antagonist, GS-2278
查看期刊：Organic Process Research & Development
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