MK-7845 was designed as a 3C-like protease inhibitor for the treatment of COVID-19. To enable a rapid kilo-scale delivery of MK-7845 to accelerate its First-in-Human studies, we developed a fit-for-purpose process to produce two key building blocks in less than two months. The key discoveries were a highly diastereoselective Ellman addition route for β-aminoamide 6 and crystallization isolation methods to produce 6 and acid 9 with good quality control.

中文翻译：

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MK-7845 作为潜在的 COVID-19 疗法的早期公斤级交付：关键中间体的快速工艺开发


MK-7845 被设计为一种类 3C 蛋白酶抑制剂，用于治疗 COVID-19。为了能够快速交付公斤级的 MK-7845，以加速其首次人体研究，我们开发了一种适合用途的工艺，可在不到两个月的时间内生产出两个关键的构建模块。关键发现是β-氨基酰胺6的高度非对映选择性埃尔曼加成路线以及在良好质量控制下生产6和酸9的结晶分离方法。