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Kilo-Scale-Enabled Route toward PF-07907063

有机合成与工艺文献分享 2025-05-29 05:19
文章摘要
本文介绍了PF-07907063的合成路线优化过程。PF-07907063是一种II型脑渗透性cMET抑制剂，最初的药物化学路线需要11步合成关键中间体3-吡唑基环丁胺24。研究团队开发了第二代和第三代路线，分别采用脱氧光氧化还原镍双催化和镍催化还原交叉偶联反应。研究发现第三代路线中NHP酯28和碘代吡唑29的偶联反应具有良好的放大性。通过优化反应条件，如使用二甲基缩酮36和催化量的甲磺酸，显著提高了亚胺形成反应的效率。此外，通过优化钯催化协议和开发组合工艺，降低了过程质量强度并提高了反应效率。最终，通过应用绿色化学的12项原则，成功开发出了适用于公斤级制备的改进路线。
Kilo-Scale-Enabled Route toward PF-07907063
查看文献： Kilo-Scale-Enabled Route toward PF-07907063, a Type II Brain Penetrant cMET Inhibitor
查看期刊：Organic Process Research & Development
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