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Commercial Route Development Toward PF-07265807 (1)

有机合成与工艺文献分享 2025-06-23 08:28
文章摘要
本文介绍了PF-07265807的商业路线开发，这是一种选择性小分子MERTK和AXL抑制剂，在体内表现出对AXL和MERTK磷酸化的强效活性，被开发为治疗晚期或转移性实体瘤的潜在药物。文章详细描述了3-碘代氮杂吲唑2的不良九步线性合成和尿嘧啶羧酸起始原料5的五步合成。研究发现，N1-氮杂吲唑保护在最终的酰胺化步骤中并非必要，因此研究重点转向寻找新的路线来获取未保护的3-丙氨醇取代的氮杂吲唑核心19和尿嘧啶羧酸5。此外，文章还探讨了三种收敛性方法用于合成尿嘧啶羧酸5。
Commercial Route Development Toward PF-07265807 (1)
查看文献： Commercial Route Development Toward PF-07265807, an AXL-MER Inhibitor Oncology Candidate
查看期刊：Organic Process Research & Development
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