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Process for a Highly Substituted Quinazoline Core (2)

有机合成与工艺文献分享 2025-11-18 07:20
文章摘要
本文研究了高取代喹唑啉核心结构的合成工艺优化。背景显示使用NCS进行芳香族氯化时存在反应活性不足的问题。研究通过添加无水HCl（0.25当量）在DMF中实现了-5°C低温下的高效区域选择性氯化，收率达87%。实验发现TMSCl等添加剂的效果不稳定，水分含量是关键参数。研究重点解决了卤化副产物20和21的形成问题，通过快速加料（<4小时）和低温控制（-10至0°C）可有效抑制杂质。机理研究表明副反应可能涉及氯离子对缺电子芳烃的亲核加成。结论表明该工艺实现了低温高效合成，并为杂质控制提供了有效策略。
Process for a Highly Substituted Quinazoline Core (2)
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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