Palladium-mediated conversion of para-aminoarylboronic esters into para-aminoaryl- 11C-methanes

Valdemar Lykke Andersen, Matthias Manfred Herth, Szabolcs Lehel, Gitte Moos Knudsen, Jesper Langgaard Kristensen

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    Abstract

    Cross-couplings are an alternative to conventional 11C-methylations which are generally employed in PET tracer synthesis. Therefore, we set out to develop a general procedure for the synthesis of para-11CH3 labeled aromatic amines from the corresponding para-aminoarylboronic esters in the presence of free amines. Aryl boronic esters containing primary, secondary, and tertiary amines were successfully converted into corresponding labeled methyl derivatives in suf¿cient radiochemical yield to apply this
    method for tracer development. This procedure was applied to the labeling of CIMBI-712, a promising
    candidate for the in vivo imaging of the 5-HT 7 receptor in the CNS
    Original languageEnglish
    JournalTetrahedron Letters
    Volume54
    Issue number3
    Pages (from-to)213-216
    Number of pages4
    ISSN0040-4039
    DOIs
    Publication statusPublished - 2013

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