Radiobromination of closo-carboranes using palladium-catalyzed halogen exchange

Karl Johan Winberg, Eskender Mume, Vladimir Tolmachev, Stefan Sjöberg

    Research output: Contribution to journalArticlepeer-review

    11 Citations (Scopus)

    Abstract

    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.

    Original languageEnglish
    Pages (from-to)195-202
    Number of pages8
    JournalJournal of Labelled Compounds and Radiopharmaceuticals
    Volume48
    Issue number3
    DOIs
    Publication statusPublished - Mar 2005

    Keywords

    • [Br]bromide
    • Carboranes
    • Catalyst
    • Halogen exchange
    • Labelling
    • Palladium

    ASJC Scopus subject areas

    • Analytical Chemistry
    • Biochemistry
    • Radiology Nuclear Medicine and imaging
    • Drug Discovery
    • Spectroscopy
    • Organic Chemistry

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