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

Research output: Contribution to journalJournal articleResearchpeer-review

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

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

ID: 43227214