The synthesis of non-steroidal estrogen receptor binding compounds labeled with 80mBr

R. H. Seevers, R. C. Mease, A. M. Friedman, E. R. Desombre

Research output: Contribution to journalArticlepeer-review

Abstract

Estrogen receptor (ER) binding radiopharmaceuticals have potenial for use in the diagnosis and treatment of cancers of the female reproductive system. Two triphenylethylene derivatives based on the structure of hydroxytamoxifen 4, a high ER binding metabolite of tamoxifen 5, have been prepared: 1-(4-dimethylaminoethoxy)phenyl]-1-(4-hydroxy)phenyl-2-bromo-2-phenylethylene 2 and 1,1-bis(p-hydroxyphenyl)-2-bromo-2-phenylethylene 3. Both 2 and 3 bind strongly to the ER. Compound 3 has been labeled in modest yield by direct bromination with 80mBr, which was produced by the 83Kr (d,nα) reaction. Radiolabeled 22, a dimethoxy precursor of 3, has been prepared in yields ranging between 40 and 60% by a bromination destannylation reaction.

Original languageEnglish (US)
Pages (from-to)483-495
Number of pages13
JournalInternational Journal of Radiation Applications and Instrumentation.
Volume13
Issue number4
DOIs
StatePublished - 1986
Externally publishedYes

ASJC Scopus subject areas

  • Medicine(all)

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