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Radiobromination of closo-dodecaborate anion. Aspects of labelling chemistry in aqueous solutions using Chloramine-T
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology.
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2002 (English)In: Radiochimica Acta, ISSN 0033-8230, E-ISSN 2193-3405, Vol. 90, no 4, 229-235 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2002. Vol. 90, no 4, 229-235 p.
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Organic Chemistry
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URN: urn:nbn:se:uu:diva-62500OAI: oai:DiVA.org:uu-62500DiVA: diva2:90411
Available from: 2008-06-16 Created: 2008-06-16 Last updated: 2017-11-30Bibliographically approved

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Tolmachev, VladimirLundqvist, HansSjöberg, Stefan

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Department of Oncology, Radiology and Clinical ImmunologyDepartment of Biochemistry and Organic Chemistry
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