Copper-Mediated Radiosynthesis of [18F]Rucaparib

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 F-18-isotopologue of rucaparib by applying a copper-mediated nucleophilic F-18-fluorodeboronation. The most successful approach features an aldehydic boronic ester precursor that is subjected to reductive amination post-F-18-labeling and affords [F-18]rucaparib with an activity yield of 11% +/- 3% (n = 3) and a molar activity (Am) up to 30 GBq/mu mol. Preliminary in vitro studies are presented.

Automated summary

This study presents two strategies for accessing the F-18-isotopologue of rucaparib using a copper-mediated nucleophilic F-18-fluorodeboronation. The most successful approach involves an aldehydic boronic ester precursor and reductive amination post-F-18-labeling, resulting in [F-18]rucaparib with a high activity yield and molar activity. Preliminary in vitro studies showed promising results.