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Radiobromination of closo ‐carboranes using palladium‐catalyzed halogen exchange
Author(s) -
Winberg Karl Johan,
Mume Eskender,
Tolmachev Vladimir,
Sjöberg Stefan
Publication year - 2005
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.914
Subject(s) - carborane , chemistry , halogen , boron , catalysis , palladium , yield (engineering) , toluene , bromine , radiochemistry , medicinal chemistry , organic chemistry , alkyl , materials science , metallurgy
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 [ 76 Br]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.