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A Key Intermediate of KRASG12C Inhibitor GH35

有机合成与工艺文献分享 2025-12-24 07:30
文章摘要
本文背景为GH35作为一种强效的不可逆共价KRASG12C抑制剂，正处于针对晚期实体瘤患者的I期临床试验阶段。研究目的是基于原有合成路线，进行初步工艺优化，以制备百克级GH35用于动物研究。结论包括：在甲苯中无需碱即可顺利进行酰化反应，且酰氯1-1用量可降至1.1当量；三乙胺/THF体系使反应均相进行，仍用于环化反应；拆分过程中水分含量对效率至关重要；筛选出65°C为最佳反应温度，5小时内完成转化且杂质谱最优；尝试替代路线时发现手性纯度在偶联反应中略有下降；最终采用已确定的催化剂体系将溴化物16转化为腈17。
A Key Intermediate of KRASG12C Inhibitor GH35
查看文献： Development of a Practical Telescoped Process to Prepare (P)-7-(2-Amino-6-fluorophenyl)-4-hydroxy-6-(trifluoromethyl)pyrido[3,4-d]pyrimidin-8(7H)-one: a Key Intermediate of KRASG12C Inhibitor GH35
查看期刊：Organic Process Research & Development
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