A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging. Academic Article uri icon

abstract

  • The unnatural isotope fluorine-18 ((18)F) is used as a positron emitter in molecular imaging. Currently, many potentially useful (18)F-labeled probe molecules are inaccessible for imaging because no fluorination chemistry is available to make them. The 110-minute half-life of (18)F requires rapid syntheses for which [(18)F]fluoride is the preferred source of fluorine because of its practical access and suitable isotope enrichment. However, conventional [(18)F]fluoride chemistry has been limited to nucleophilic fluorination reactions. We report the development of a palladium-based electrophilic fluorination reagent derived from fluoride and its application to the synthesis of aromatic (18)F-labeled molecules via late-stage fluorination. Late-stage fluorination enables the synthesis of conventionally unavailable positron emission tomography (PET) tracers for anticipated applications in pharmaceutical development as well as preclinical and clinical PET imaging.

published proceedings

  • Science

altmetric score

  • 33.764

author list (cited authors)

  • Lee, E., Kamlet, A. S., Powers, D. C., Neumann, C. N., Boursalian, G. B., Furuya, T., ... Ritter, T.

citation count

  • 358

complete list of authors

  • Lee, Eunsung||Kamlet, Adam S||Powers, David C||Neumann, Constanze N||Boursalian, Gregory B||Furuya, Takeru||Choi, Daniel C||Hooker, Jacob M||Ritter, Tobias

publication date

  • November 2011