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Process for a Highly Substituted Quinazoline Core (3)

有机合成与工艺文献分享 2025-11-19 06:47
文章摘要
本文研究喹唑啉-2,4(1H,3H)-二酮的合成工艺优化。背景基于Mizuno团队报道的二氧化碳环化方法，研究目的旨在解决工业化生产中二甲基亚砜残留导致的二聚化副反应问题。通过实验发现当DMSO残留量达5000 ppm时会产生约5%的二聚体，为此开发了分步温控工艺：先在20-35°C缓慢加入DIPEA进行磷酸化并添加0.25当量水，再升温至70°C实现2小时内快速氯化。该方案将二聚化副反应降至最低，使过程控制纯度达到≥97.0%，最终获得93-94%收率和>99.0% HPLC纯度的高品质产物。
Process for a Highly Substituted Quinazoline Core (3)
查看文献： Development of a Streamlined Manufacturing Process for the Highly Substituted Quinazoline Core Present in KRAS G12C Inhibitor Divarasib
查看期刊：Organic Process Research & Development
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