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Scalable Atroposelective Synthesis of MRTX1719 (4)

有机合成与工艺文献分享 2025-11-27 06:56
文章摘要
本文背景介绍自1880年代以来，通过2-酰基苯甲酸与肼缩合制备取代酞嗪酮的经典方法。研究目的旨在开发MRTX1719的规模化不对称合成路线，重点解决传统Gabriel方法中氨基保护/脱保护步骤繁琐及副产物难分离的问题。通过采用定向邻位金属化策略，探索了含胺双碳亲电试剂的反应可行性，发现有机锂试剂因强碱性导致酸基反应占主导。最终利用Knochel课题组开发的CuCl•2LiCl活化有机锌试剂，成功实现与乙酰氯的清洁偶联，获得未取代酮类化合物21h（收率>90%），为关键α-氨基酮结构的构建提供了新途径。
Scalable Atroposelective Synthesis of MRTX1719 (4)
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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