Radiobromination of closo-dodecaborate anion. Aspects of labelling chemistry in aqueous solution using Chloramine-T

Vladimir Tolmachev, Alexander Bruskin, Hans Lundqvist, Igor Sivaev, Stefan Sjöberg, Alexander Bruskin, Igor Sivaev

Research output: Contribution to journalArticlepeer-review

33 Citations (Scopus)

Abstract

Closo-dodecaborate dianion is a three-dimensional aromatic inorganic molecule, which can be easily halogenated forming a stable halogen-boron bond. Derivatives of closo-dodecaborate were considered as a convenient chemical form of delivery of enriched 10B to malignant tumors for boron neutron capture therapy (BNCT). Some properties of closo-dodecaborate (hydrophilicity, strength of halogen-boron bond, charge at lysosomal pH) make it attractive as a potential prosthetic group for attachment of radioactive halogens to tumor-targeting proteins. Bromine radioisotopes possess a variety of useful nuclear characteristics, and can be used in different areas of clinical diagnostics and therapy. In this work, a basic chemistry of closo-dodecaborate radiobromination was studied. It was found, that di(triethylamonium) dodecahydro-closo-dodecaborate can be labelled in high yield, more then 90%, in a wide pH range. By decreasing the pH, the bromination can be directed to closo-dodecaborate in the presence of phenolic compounds. The results of the study indicate a possibility of using the radioactive bromine label for investigation of pharmacokinetics of boronated compounds for BNCT.

Original languageEnglish
Pages (from-to)229-235
Number of pages7
JournalRadiochimica Acta
Volume90
Issue number37347
DOIs
Publication statusPublished - 2002
Externally publishedYes

Keywords

  • Aqueous media
  • Bromo-undecahydoro-closo-dodecaborate
  • Chloramine-T
  • Dodecahydro-closo-dodecaborate (2-)
  • Radiobromination

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry

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