Next Generation Copper Mediators for the Efficient Production of ¹⁸ F-Labeled Aromatics.

ABSTRACT: Cu-mediated radiofluorination is a versatile tool for the preparation of ¹⁸ F-labeled (hetero)aromatics. In this work, we systematically evaluated a series of complexes and identified several generally applicable mediators for highly efficient radiofluorination of aryl boronic and stannyl substrates. Utilization of these mediators in nBuOH/DMI or DMI significantly improved ¹⁸ F-labeling yields despite use of lower precursor amounts. Impressively, application of 2.5 μmol aryl boronic acids was sufficient to achieve ¹⁸ F-labeling yields of up to 75 %. The practicality of the novel mediators was demonstrated by efficient production of five PET-tracers and transfer of the method to an automated radiosynthesis module. In addition, (S)-3-[¹⁸ F]FPhe and

SUBMITTER: Hoffmann C 

PROVIDER: S-EPMC10100267 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature