Synthesis of high specific activity 80mBr and 123I labeled 5‐halodeoxyuridines and other 80mBr compounds for the study of auger electron toxicity

Rc Mease, Sj Gatley, Am Friedman

Research output: Contribution to journalArticle

Abstract

Convenient preparations of 80mBr and 123I‐labeled 5‐halodeoxyuridines, required for basic investigations of Auger electron radiotoxicity, are described. These radioactive thymidine analogs were synthesized from deoxyuridine, radiohalide and N‐chlorosuccinimide in dilute sulfuric acid. Yields were 50–60% for 80mBr and 60–70% for 123I. Apparent specific radioactivities (based on UV absorption under the radioactive HPLC peaks) were 150–550 Ci/mmol and over 2000 Ci/mmol for 80mBr and 123I, respectively. 5‐[80mBr]bromouracil was produced in 89% yield when uracil was used. [80mBr]Bromoantipyrine was produced in higher yield and specific activity using peroxyacetic acid, rather than N‐chlorosuccinimide as oxidant (90% and 4,000 Ci/mmol versus 50% and 2000 Ci/mmol).

Original languageEnglish (US)
Pages (from-to)393-403
Number of pages11
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume29
Issue number4
DOIs
StatePublished - Apr 1991
Externally publishedYes

Keywords

  • 5‐bromo‐2′‐deoxyuridine
  • 5‐iodo‐2′‐deoxyuridine
  • Auger electron
  • Br
  • I
  • bromoantipyrine

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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