Method for synthesizing Iguratimod key intermediate

The invention relates to preparation of Iguratimod key intermediate 3-amino-4-phenoxy anisole. The chemical reaction formula of the method is shown in the specification. According to the method, ammonium formate is taken as a hydrogen source, palladium carbon hydroxide is taken as a catalyst, and 3-...

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Bibliographische Detailangaben
Hauptverfasser: LONG XIGUO, WANG DONG, XU LINYU, JIANG HAITING, HU KAI, LUO PENG, QIAO WEN, HU GANG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to preparation of Iguratimod key intermediate 3-amino-4-phenoxy anisole. The chemical reaction formula of the method is shown in the specification. According to the method, ammonium formate is taken as a hydrogen source, palladium carbon hydroxide is taken as a catalyst, and 3-nitro-4-phenoxy anisole (2) is reduced into 3-amino-4-phenoxy anisole (1). The structure of the target product is confirmed by HPLC, 1H-NMR, MS and the like. The improved reduction process avoids special hydrogenation pressurization reaction, reduces the safety risk and the production cost, and has high commercial value. 本发明涉及一种艾拉莫德关键中间体3-氨基-4-苯氧基苯甲醚的制备,所述方法的化学反应式如下所示。以甲酸铵作为氢源,氢氧化钯碳为催化剂,将3-硝基-4-苯氧基苯甲醚(2)还原成3-氨基-4-苯氧基苯甲醚(1)。目标产物结构经HPLC、1H-NMR和MS等确证。改进后的还原工艺,避开了氢化加压特种反应,降低了安全风险和生产成本,具有较高的商业化价值。