Preparation method of Vonoprazan fumarate

The invention provides a preparation method of Vonoprazan fumarate, the preparation method adopts a new synthesis route, o-fluoroacetophenone and ethyl cyanoacetate are adopted as raw materials, a final product is obtained through seven-step reaction, an intermediate product 5-(2-fluorophenyl)-1H-py...

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Hauptverfasser: WANG WEI, ZHANG FENGDE, DONG LIANGJUN, HAN DEXU, LI XIAOHUI, LI HONGCHENG, SUN YANGE, ZHANG ZUODAO, CHU YAFEI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a preparation method of Vonoprazan fumarate, the preparation method adopts a new synthesis route, o-fluoroacetophenone and ethyl cyanoacetate are adopted as raw materials, a final product is obtained through seven-step reaction, an intermediate product 5-(2-fluorophenyl)-1H-pyrrole-3-carboxylic acid ethyl ester is not subjected to hydrogenation reaction, the yield is high, and the yield is high. The synthesis steps can be obviously shortened, the reduction operation is reduced, the potential impurities are fewer, the product quality is improved, and the production cost is more competitive. 本发明提供了一种富马酸伏诺拉生的制备方法,所述制备方法采用新的合成路线,采用邻氟苯乙酮与氰基乙酸乙酯为原料,经过7步反应得到最终产品,中间产物5-(2-氟苯基)-1H-吡咯-3-羧酸乙酯之后不采用加氢反应,可以显著缩短合成步骤,减少还原操作,潜在杂质更少,提升产品质量、生产成本更有竞争力。