Copper-Mediated Radiosynthesis of [¹⁸F]Rucaparib

This is the authors' abstract. We don't add key points for this paper.

The poly(ADP-ribose) polymerase (PARP) inhibitor rucaparib is used in the clinic to treat BRCA -mutated cancers. Herein, we report two strategies to access the 18 F-isotopologue of rucaparib by applying a copper-mediated nucleophilic 18 F-fluorodeboronation. The most successful approach features an aldehydic boronic ester precursor that is subjected to reductive amination post- 18 F-labeling and affords [ 18 F]rucaparib with an activity yield of 11% ± 3% ( n = 3) and a molar activity ( A m ) up to 30 GBq/μmol. Preliminary in vitro studies are presented.