Abstract
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 mixture of Z/ E isomers that was re-subjected to HPLC separation. In this way, most of the undesired ( E)-isomer could be readily converted to the desired ( Z)-isomer providing quick access to over 200 mg quantities of pure endoxifen ( Z-isomer), a potent antiestrogenic metabolite of tamoxifen traditionally used in breast cancer treatment.
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