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

• Published in: Radiochimica acta Vol. 90; no. 4; pp. 229 - 235
• Main Authors: Tolmachev, Vladimir, Bruskin, A., Sivaev, Igor, Lundqvist, Hans, Sjöberg, Stefan
• Format: Journal Article
• Language: English
• Published: De Gruyter Oldenbourg 01.04.2002
• ISSN: 0033-8230; 2193-3405
• DOI: 10.1524/ract.2002.90.4_2002.229

-dodecaborate dianion is a three-dimensional aromatic inorganic molecule, which can be easily halogenated forming a stable halogen-boron bond. Derivatives of -dodecaborate were considered as a convenient chemical form of delivery of enriched B to malignant tumors for boron neutron capture therapy (BNCT). Some properties of -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 -dodecaborate radiobromination was studied. It was found, that di(triethylamonium) dodecahydro- -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 -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.