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Fit-for-Purpose Synthesis of a KRASG12C Covalent Inhibitor

有机合成与工艺文献分享 2025-11-13 06:52
文章摘要
本文背景为开发KRASG12C共价抑制剂作为癌症治疗新方法。研究目的旨在建立适合工业化生产的立体化学纯中间体(R,R,S)-9的合成路线，重点改进了关键手性中间体(R)-4的不对称合成方法。通过系统筛选发现SimplePHOX催化剂C1在二烯不对称氢化反应中表现出最佳转化率、区域选择性和对映体过量值，并进一步探索了底物适用范围。最终成功开发出基于改进催化剂的(R)-4合成路线，并重新评估了使用芳基硼酸14的Hayashi芳基化反应，为KRASG12C抑制剂的工业化生产提供了可行路径。
Fit-for-Purpose Synthesis of a KRASG12C Covalent Inhibitor
查看文献： Fit-for-Purpose Synthesis of a KRASG12C Covalent Inhibitor, via a Diastereoselective Hayashi Arylation
查看期刊：Organic Process Research & Development
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