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Selective Metalation of Functionalized Quinazolines

有机合成与工艺文献分享 2025-11-10 08:34
文章摘要
本文研究背景为喹唑啉环C6、C7和C8位多卤化存在的固有挑战，研究目的是开发替代合成方案以实现后期阶段溴化反应。通过采用TMP Knochel-Hauser碱和Zn-TMP碱实现C7位选择性金属化，与Br2Cl4C2反应获得良好转化率，并进一步通过Negishi交叉偶联反应建立更直接的ARS-1620合成路径。结论表明锌酰胺碱技术可获得优异产率，为功能化喹唑啉的有机合成提供了高效方法。
Selective Metalation of Functionalized Quinazolines
查看文献： Selective Metalation of Functionalized Quinazolines to Enable Discovery and Advancement of Covalent KRAS Inhibitors
查看期刊：Organic Process Research & Development
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