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Scalable Atroposelective Synthesis of MRTX1719 (3)

有机合成与工艺文献分享 2025-11-26 08:03
文章摘要
本文背景聚焦于开发不依赖贵金属催化的新型有机合成方法，以制备关键中间体频哪醇硼酸酯2。研究目的旨在探索卤素-金属交换和光催化两种替代化学方法，重点优化光催化硼化反应条件。通过系统条件筛选，最终确定以吩噻嗪为有机催化剂、390nm光照、乙腈回流的最佳反应体系，在克级规模上实现81%的转化率。研究结论表明光催化法成功实现了氯酞嗪酮类底物的硼基化，为MRTX1719的规模化合成提供了更高效、经济的工艺路线，同时有效替代了传统繁琐的Gabriel合成序列。
Scalable Atroposelective Synthesis of MRTX1719 (3)
查看文献： Scalable Atroposelective Synthesis of MRTX1719: An Inhibitor of the PRMT5/MTA Complex
查看期刊：Organic Process Research & Development
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