title: Automated synthesis of 4-[(18)F]fluoroanisole, [(18)F]DAA1106 and 4-[(18)F]FPhe using Cu-mediated radiofluorination under "minimalist" conditions.
abstract: The application of the "minimalist" approach to Cu-mediated radiofluorination allows the efficient preparation of (18)F-labeled arenes regardless of their electronic properties. The implementation of this methodology on a commercially available synthesis module (hotbox(three), Scintomics, Germany) enabled the automated production of 4-[(18)F]fluoroanisole as well as the clinically relevant PET-tracers, 4-[(18)F]FPhe and [(18)F]DAA1106, in radiochemical yields of 41-61% and radiochemical purities of >95% within 30-60min. These results demonstrated the high efficacy and versatility of the developed method that will open up opportunities for a broad application of Cu-mediated radiofluorination in PET-chemistry.
authors.affiliation: Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany.
authors.forename: Johannes
authors.initials: J
authors.lastname: Zischler
authors.affiliation: Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany.
authors.forename: Philipp
authors.initials: P
authors.lastname: Krapf
authors.affiliation: Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany.
authors.forename: Raphael
authors.initials: R
authors.lastname: Richarz
authors.affiliation: Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany.
authors.forename: Boris D
authors.initials: BD
authors.lastname: Zlatopolskiy
authors.affiliation: Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany. Electronic address: bernd.neumaier@uk-koeln.de.
authors.forename: Bernd
authors.initials: B
authors.lastname: Neumaier
keywords: Automated radiosynthesis; Cu-mediated radiolabeling; Minimalist approach; PET-tracers; [(18)F]Fluoride