Novel copper mediators for the efficient production of 18F-labeled aromatics

Abstract

To reduce the precursor amounts required for Cu-mediated radiofluorination, a series of new mediators for the ¹⁸F-labeling of aryl boronic and stannyl substrates was identified through a systematic evaluation of various copper complexes. Under optimized reaction conditions, application of these mediators significantly improved the ¹⁸F-labeling yields compared to conventional Cu(Py)₄(OTf)₂ despite the use of reduced precursor amounts. The practicality of the new mediators was demonstrated by the efficient production of several established and emerging PET tracers as well as transfer of the optimized protocol to an automated radiosynthesis module.

Hoffmann, C.; Kolks, N.; Smets, D.; Haseloer, A.; Gröner, B.; Urusova, E.; Endepols, H.; Neumaier, F.; Ruschewitz, U.; Klein, A.; Neumaier, B.; Zlatopolskiy, B. D.

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

Chemistry - a European journal 2023, 29(2).