Methodology for the synthesis and specific activity determination of 16α-[77Br]-Bromoestradiol-17 β and 16α-[77Br]-11 β-methoxyestradiol-17 β, Two estrogen receptor-binding radiopharmaceuticals

Stephen G. Senderoff, Karen D. McElvany, Kathyrn E. Carlson, Daniel F. Heiman, John A. Katzenellenbogen, Michael J. Welch

Research output: Contribution to journalArticlepeer-review


16α-[77Br]-Bromoestradiol-17β (3a) has been synthesized from estrone enol diacetate (1) by bromination with Na 77Br and hydrogen peroxide-acetic acid, followed by reduction with lithium aluminum hydride to give a mixture of 16α-[77Br]-bromoestradiol-17β (3a) and 16α-[77Br]-bromoestradiol-17α (3a) from which the desired epimer (3a) can be obtained in 50% overall radiochemical yield (from Na77Br) by HPLC. Analogous procedures can be used in the preparation of 16α-[77Br]-bromo-11β-methoxyestradiol-17β. (4a) The effective specific activities of these radiopharmaceuticals, determined by binding to the uterine estrogen receptor, are 900-1500 Ci/mmol. Both have high affinity and good binding selectivity for the estrogen receptor and are useful as imaging agents for mammary tumors.

Original languageEnglish (US)
Pages (from-to)545-551
Number of pages7
JournalThe International Journal Of Applied Radiation And Isotopes
Issue number7
StatePublished - Jul 1982

ASJC Scopus subject areas

  • Radiation
  • Nuclear Energy and Engineering
  • Radiology Nuclear Medicine and imaging


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