Bazedoxifene impurity synthesis method

The present invention provides a synthesis method for synthesizing bazedoxifene impurity, wherein 4-hydroxyphenethyl alcohol is adopted as a raw material, benzyl chloride is adopted to protect phenolic hydroxyl, thionyl chloride reacts with phenethyl alcohol to produce benzyl chloride, the benzyl ch...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: LIU YA'NAN, RAN ZHAOJIN, YAN QIQIANG
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:The present invention provides a synthesis method for synthesizing bazedoxifene impurity, wherein 4-hydroxyphenethyl alcohol is adopted as a raw material, benzyl chloride is adopted to protect phenolic hydroxyl, thionyl chloride reacts with phenethyl alcohol to produce benzyl chloride, the benzyl chloride reacts with an intermediate 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole, and the benzyl protection is removed through catalytic hydrogenation of palladium-carbon to obtain the bazedoxifene impurity. According to the present invention, the method does not require the special reagent, and the required raw materials are cheap and easily available. The structure formula of the bazedoxifene impurity is defined in the instruction.