Exploration of alcohol-enhanced Cu-mediated radiofluorination toward practical labeling.

ABSTRACT: Copper-mediated nucleophilic radiofluorination using boronic precursors is a promising, general method to label aromatic compounds with [¹⁸ F]fluoride. However, in various reports, large amounts of precursor (60 μmol) were needed to achieve high radiochemical conversions (RCCs), which is neither ideal nor practical for the preparation of ¹⁸ F radiopharmaceuticals. To investigate this matter, we studied alcohol-enhanced Cu-mediated nucleophilic radiofluorination using a variety of model reactions in which we varied the concentration of [¹⁸ F]fluoride (no carrier added or isotope diluted) and the amount of precursor, base, and Cu(OTF)₂ (Py)₄ . We found that lower amounts of precursors (e.g., 15 μmol) could be used and that the amount of

SUBMITTER: Zhou D 

PROVIDER: S-EPMC8727449 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature