托法替尼合成路线图解

Graphical synthetic routes of tofacitinib

目的:通过分析现有的托法替尼合成方法找到适合工业化生产的路线。方法:对托法替尼的合成路线进行总结。结果:路线1b条件温和,总收率较高,更加适于工业化生产。结论:在得到关键片段后,经后续反应得到托法替尼。

Objective： To review the existing synthetic routes of tofacitinib, and find the suitable route for industrialization. Methods： We summarized the various synthetic process of tofacitinib. Results：The route lb, with the moderate reaction conditions and a high total yield, shows more favorable in manufacturing scale. Conclusion： After getting the key fragments and by the subsequent reaction we can get tofacitinib.