- High affinity fluorescent ligands for the estrogen receptor
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Fluorescent binders of the estrogen receptor (ER) are used in binding assays and in detection or imaging studies. However, fluorescence labelling of ER ligands usually leads to substantial decreases in binding affinity. In this study, we describe the deve
- Abendroth, Frank,Solleder, Marthe,Mangoldt, Dorothea,Welker, Pia,Licha, Kai,Weber, Marcus,Seitz, Oliver
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p. 2157 - 2166
(2015/04/14)
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- Triphenylethylenes, process for their production, pharmaceutical preparations that contain these triphenylethylenes as well as their use for the production of pharmaceutical agents
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This invention describes the new triphenylethylenes of general formula I STR1 in which n means an integer from 1 to 10, R' means a sulfur-containing organic radical, R" means a hydrogen atom, an iodine atom or a hydroxy groups, E means a hydrogen atom, G
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- The Use of the Perfluorotolyl Protecting Group in the Synthesis of Pure Z and E Isomers of 4-Hydroxytamoxifen -1-(4-hydroxyphenyl)-2-phenyl-1-butene>
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The perfluorotolyl protecting group has been used in the synthesis of pure Z and E isomers of 4-hydroxytamoxifen (4a), a potent metabolite of the anticancer drug, tamoxifen (1a). 4-(Perfluorotolyloxy)phenyl magnesium bromide underwent addition to the carbonyl group of the easily prepared versatile ketone, 1--2-phenyl-1-butanone (7), without affecting the chloroethoxy group.Acid catalysed dehydration of the resulting carbinol gave a 1:1 mixture of isomeric ethers, (6a) and (6b), that were easily separated by chromatography and respectively converted to the Z (4a) and E (4b) isomers of 4-hydroxytamoxifen.The property of the perfluorotolyl function in enabling the separation of geometrical isomers is attributed to a combination of its lipophilicity and electron withdrawal.
- McCague, Raymond
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p. 771 - 793
(2007/10/02)
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