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

  • Vladimir Tolmachev , A. Bruskin , Igor Sivaev , Hans Lundqvist and Stefan Sjöberg
Published/Copyright: September 25, 2009

Summary

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.

Received: 2001-8-14
Accepted: 2001-12-10
Published Online: 2009-9-25
Published in Print: 2002-4-1

© Oldenbourg Wissenschaftsverlag, München

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