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Feasibility of palladium catalysed isotopic exchange between [125I]iodide and 2-iodo-para-carborane
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology. (BMS)
2003 (English)In: Journal of labelled compounds & radiopharmaceuticals, ISSN 0362-4803, E-ISSN 1099-1344, Vol. 46, no 7, 623-631 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2003. Vol. 46, no 7, 623-631 p.
Keyword [en]
isotopic exchange, 2-iodo-para-carborane, [125I]iodide, labeling, palladium
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-64294DOI: 10.1002/jlcr.702OAI: oai:DiVA.org:uu-64294DiVA: diva2:92205
Available from: 2008-10-17 Created: 2008-10-17 Last updated: 2014-03-05Bibliographically approved

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Tolmachev, Vladimir
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Department of Oncology, Radiology and Clinical Immunology
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