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Evolution of the Process to an Advanced GPR40 Agonist (3)

有机合成与工艺文献分享 2025-04-17 07:36
文章摘要
本文主要探讨了高级GPR40激动剂(3)的合成工艺优化过程。研究背景涉及传统Weinreb酰胺合成方法的局限性，如需要使用Me3Al试剂和低温条件(-78°C)等。研究目的是开发更温和、高效且能避免α-立体中心差向异构化的合成方法。通过使用LiOH/H2O2温和条件实现羧酸的清洁转化，并采用LDBBA替代DIBAL-H解决了低温要求和差向异构化问题。结论表明，改进后的Ando修饰HWE烯化反应方案更具优势，使用Triton B作为碱避免了18-crown-6的使用，且Touchard等人报道的改进方法使烯化反应能在室温下进行，大大优化了合成工艺。
Evolution of the Process to an Advanced GPR40 Agonist (3)
查看文献： Evolution of the Synthetic Process to an Advanced GPR40 Agonist
查看期刊：Organic Process Research & Development
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