Momelotinib是Janus激酶的选择性抑制剂,用于治疗中高风险骨髓纤维化.为了解决现有合成方法存在的成本高、反应条件严苛、收率偏低和废料对环境污染严重等问题,以1-氟-4-硝基苯为起始原料,经取代、还原、Pinner、与DMF-DMA 缩合、环合、水解和酰化反应合成目标化合物 Momelotinib,总收率为 55.04%,纯度为99.45%.Momelotinib的化学结构经1 H NMR、13 C NMR和MS(ESI)确证.上述合成路线试剂成本低、操作简便、收率高且绿色环保,适合工业化生产.
Abstract
Momelotinib is a selective Janus kinase inhibitor and can be used to treat moderate or high-risk myelofibrosis.In order to solve the problems of reported synthetic methods such as high cost,strict reaction conditions,low yield and serious environmental pollution,using 1-fluoro-4-nitrobenzene as the starting material,the target compound Momelotinib was synthesized by substitution,reduction,Pinner,condensation with DMF-DMA,cyclization,hydrolysis and acylation reactions.The total yield was 55.04%and the purity was 99.45%.The chemical structure of Momelotinib was confirmed by 1 H NMR,13 C NMR and MS(ESI).The above synthetic route showed the characteristics of low rea-gent cost,simple operation,high yield and environmental friendly,which is suitable for industrial pro-duction.
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