Synthesis method of semetinib

The invention relates to a synthesis method of simetinib. According to the method, diethoxymethane is creatively adopted as a ring closing reactant, and two-step reaction of ring closing reaction and methylation is combined into one step, so the yield is very high, and the number of reaction steps i...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: FAN ZHAOZE, LIU SHAOQUN, CHEN LONG, HU RENJUN, DUN WEI, YU YANPING, LI XURONG, HUANG XIANGQUAN
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention relates to a synthesis method of simetinib. According to the method, diethoxymethane is creatively adopted as a ring closing reactant, and two-step reaction of ring closing reaction and methylation is combined into one step, so the yield is very high, and the number of reaction steps is reduced. According to the synthetic route disclosed by the invention, the semitinib is synthesized through three-step reaction, the post-treatment of the synthetic method does not need column chromatography separation, and the reaction product is directly separated out and dried. 本发明涉及一种司美替尼的合成方法。本发明创新性的采用二乙氧基甲烷作为关环反应物,将关环反应和甲基化两步反应合并在一步,不仅产率很高,减少了反应步数。本发明的合成路线经三步反应合成得到司美替尼,其合成方法的后处理均无需柱层析分离,反应产物直接析出干燥即可。