New and practical synthetic route of momelotinib, a JAK inhibitor, is described on a decagram scale. A convergent synthetic process is adopted to prepare the methyl 4‐(2‐((4‐morpholinophenyl)amino)pyrimidin‐4‐yl) benzoate intermediate, by cyclization of 1‐(4‐morpholinophenyl)guanidine and methyl 4‐(3‐(dimethylamino)acryloyl)benzoate in high yield and mild conditions. Momelotinib is obtained in 43.2% yield over five steps and 99.1% purity (HPLC).

中文翻译：

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莫莫替尼的新实用合成

JAK抑制剂莫米罗替尼的新型实用合成路线以十克级规模描述。通过收敛合成工艺，通过环化1-（4-吗啉代苯基）胍和甲基4-（3--），制备4-（2-（（4-吗啉代苯基）氨基）嘧啶-4-基）苯甲酸甲酯中间体。 （二甲基氨基）丙烯酰基）苯甲酸酯在高产率和温和条件下。在五个步骤中获得莫洛替尼的产率为43.2％，纯度为99.1％（HPLC）。