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Manufacturing Process for Key Intermediate of Divarasib (1)

有机合成与工艺文献分享 2025-11-06 08:39
文章摘要
本文围绕抗癌药物Divarasib关键中间体1的合成工艺开发展开。背景方面，早期工艺虽已生产超100公斤中间体，但存在优化空间。研究目的旨在开发实用且可放大的合成路线，探索了收敛环化策略和Guareschi-Thorpe吡啶合成变体，但环化反应未获成功。后续重点研究通过脱氧氟化反应引入CF3基团的新方法，详细优化了2,6-二氯-4-甲基烟酸(13)的反应条件，通过控制温度至80℃以下、调整SF4当量至2.5，有效控制了氟吡啶杂质的生成。结论表明采用33wt% HBr/AcOH缓慢加料工艺，可将溴氯吡啶杂质(17)控制在0.15%以下，最终获得纯度超过97.5%的目标产物12，为工业化生产提供了可行方案。
Manufacturing Process for Key Intermediate of Divarasib (1)
查看文献： Manufacturing Process for 6-Bromo-N,N-bis(4-methoxybenzyl)-4-methyl-5-(trifluoromethyl)pyridin-2-amine, a Key Intermediate in the Synthesis of KRAS G12C Inhibitor Divarasib
查看期刊：Organic Process Research & Development
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