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Feasibility of palladium catalysed isotopic exchange between [125I]iodide and 2-iodo-para-carborane
- Eriksson, Ludvig (author)
-
- Tolmachev, Vladimir (author)
- Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS
- Sjöberg, Stefan (author)
- (creator_code:org_t)
- 2003-04-22
- 2003
- English.
- In: Journal of labelled compounds & radiopharmaceuticals. - : Wiley. - 0362-4803 .- 1099-1344. ; 46:7, s. 623-631
- Journal article (peer-reviewed)
Abstract
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- 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.
Keyword
- isotopic exchange
- 2-iodo-para-carborane
- [125I]iodide
- labeling
- palladium
- MEDICINE
- MEDICIN
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- ref (subject category)
- art (subject category)
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