1231819-50-3Relevant articles and documents
TOPICAL COMPOSITIONS AND METHODS FOR TREATMENT
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Page/Page column 83; 84, (2019/04/09)
The present disclosure provides novel topical compositions comprising endoxifen and salts and solvates thereof and methods for making the compositions. Certain compounds have been combined to make a stable topical compositions comprising endoxifen. The pr
A convenient synthesis of (Z)-4-hydroxy-N-desmethyltamoxifen (endoxifen)
Fauq, Abdul H.,Maharvi, Ghulam M.,Sinha, Dola
supporting information; experimental part, p. 3036 - 3038 (2010/07/03)
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.