Radiobromination of closo-carboranes using palladium-catalyzed halogen exchange

closo‐Carborane derivatives are often proposed as boron carriers for use in boron neutron capture therapy (BNCT) of cancer. A positron emitting radiolabel on a boron atom in such carborane compounds might facilitate pharmacokinetic studies in patients. In this paper the four iodo‐closo‐carboranes, n...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2005-03, Vol.48 (3), p.195-202
Main Authors: Winberg, Karl Johan, Mume, Eskender, Tolmachev, Vladimir, Sjöberg, Stefan
Format: Article
Language:English
Subjects:
[76Br]bromide
B derivatives
Biological and medical sciences
carboranes
catalyst
Chemistry
Contrast media. Radiopharmaceuticals
Exact sciences and technology
halogen exchange
Kemi
labelling
Medical sciences
NATURAL SCIENCES
NATURVETENSKAP
Organic chemistry
Organisk kemi
Organometalloidal and organometallic compounds
palladium
Pharmacology. Drug treatments
Preparations and properties
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Summary:closo‐Carborane derivatives are often proposed as boron carriers for use in boron neutron capture therapy (BNCT) of cancer. A positron emitting radiolabel on a boron atom in such carborane compounds might facilitate pharmacokinetic studies in patients. In this paper the four iodo‐closo‐carboranes, namely 3‐iodo‐ortho‐carborane, 9‐iodo‐ortho‐carborane, 9‐iodo‐meta‐carborane and 2‐iodo‐para‐carborane were chosen as model compounds in a study of [76Br]bromine labelling of carboranes using palladium‐catalyzed halogen exchange. It was found that within a reaction time of 40 min, the four compounds were all radio‐brominated in good to excellent yield, using Herrmann's catalyst (HC) in toluene. Copyright © 2005 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
1099-1344
DOI:10.1002/jlcr.914