Abstract
AbstractMany 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. Copyright © 2003 John Wiley & Sons, Ltd.
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