Synthesis of the E and Z isomers of the antiestrogen tamoxifen and its metabolite, hydroxytamoxifen, in tritium-labeled form
Journal Article
·
· J. Org. Chem.; (United States)
Both isomers of the potent antiestrogen tamoxifen (1,2-diphenyl-1-(4-(2-(dimethylamino)ethoxy)phenyl)-1-butene: E isomer = ICI-47699; Z isomer = ICI-46474, Nolvadex) and its metabolite, hydroxytamoxifen (1-(4-(2-(dimethylamino)ethoxy)phenyl)-1-(4-hydroxyphenyl)-2-phenyl-1-butene), have been synthesized in a high specific activity, tritium-labeled form by catalytic tritium-halogen exchange performed on brominated precursors. The synthesis of another precursor to labeled tamoxifen which would enable the incorporation of three tritium atoms into the molecule by tritium-halogen exchange is reported.
- Research Organization:
- Univ. of Illinois, Urbana
- OSTI ID:
- 6594667
- Journal Information:
- J. Org. Chem.; (United States), Vol. 47:12
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
59 BASIC BIOLOGICAL SCIENCES
TAMOXIFEN
LABELLING
TRITIUM
RADIOCHEMISTRY
CHEMICAL PREPARATION
CHEMICAL REACTION KINETICS
EXPERIMENTAL DATA
ISOMERS
METABOLITES
TRITIUM COMPOUNDS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
CHEMISTRY
DATA
HYDROGEN ISOTOPES
INFORMATION
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RADIOISOTOPES
REACTION KINETICS
SYNTHESIS
YEARS LIVING RADIOISOTOPES
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
550201 - Biochemistry- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
TAMOXIFEN
LABELLING
TRITIUM
RADIOCHEMISTRY
CHEMICAL PREPARATION
CHEMICAL REACTION KINETICS
EXPERIMENTAL DATA
ISOMERS
METABOLITES
TRITIUM COMPOUNDS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
CHEMISTRY
DATA
HYDROGEN ISOTOPES
INFORMATION
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RADIOISOTOPES
REACTION KINETICS
SYNTHESIS
YEARS LIVING RADIOISOTOPES
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
550201 - Biochemistry- Tracer Techniques