Bioorganic & medicinal chemistry letters

A convenient synthesis of (Z)-4-hydroxy-N-desmethyltamoxifen (endoxifen)

AH Fauq, GM Maharvi, D Sinha

文献索引：Fauq, Abdul H.; Maharvi, Ghulam M.; Sinha, Dola Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 10 p. 3036 - 3038

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被引用次数: 17

摘要

A mixture of the (Z)-and (E)-isomers of 4-hydroxy-N-desmethyltamoxifen was conveniently prepared in four steps. These geometrical isomers were then neatly separated by semi- preparative Reverse Phase High Performance Liquid Chromatography (RP-HPLC) using specified conditions. Additionally, the isolated E-isomer could be equilibrated in aqueous strong acid in acetonitrile or trifluoroacetic acid/dichloromethane to give a clean 1: 1 ...