Feasibility of palladium-catalyzed isotopic exchange between sodium [125I]I and 2-iodo-para-carborane

Ludvig Eriksson, Vladimir Tolmachev, Stefan Sjöberg

Research output: Contribution to journalArticlepeer-review

13 Citations (Scopus)

Abstract

Many ortho-/meta-/para-closo-carborane derivatives have been proposed for boron neutron capture therapy. However, it is difficult to follow their pharmacokinetics in patients, which creates a risk of suboptimal treatment. Adding a radioactive label to closo-carboranes may simplify pharmacokinetic studies. This paper reports on a study of the feasibility of palladium-catalyzed isotopic exchange of iodinated closo-carborane with radioisotopes of iodine. 2-iodo-para-carborane was selected as a model compound. It was shown that such isotopic exchange is possible and provides a high yield (83 ± 4.2%) after 40 min of reaction time. The reaction conditions were optimized, and it was demonstrated that the presence of tetra n-butylammonium hydrogensulfate is important in order to stabilize the catalyst and to give reproducibility of the labeling.

Original languageEnglish
Pages (from-to)623-631
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume46
Issue number7
DOIs
Publication statusPublished - Jun 2003
Externally publishedYes

Keywords

  • 2-iodo-para-carborane
  • Isotopic exchange
  • Labeling
  • Palladium
  • [I]iodide

ASJC Scopus subject areas

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

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