Copper-mediated radiosynthesis of [18F]rucaparib
<p>The poly(ADP-ribose) polymerase (PARP) inhibitor rucaparib is used in the clinic to treat <em>BRCA</em>-mutated cancers. Herein, we report two strategies to access the <sup>18</sup>F-isotopologue of rucaparib by applying a copper-mediated nucleophil...
| Main Authors: | , , , , , |
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| Format: | Journal article |
| Language: | English |
| Published: |
American Chemical Society
2021
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| Summary: | <p>The poly(ADP-ribose) polymerase (PARP) inhibitor rucaparib is used in the clinic to treat <em>BRCA</em>-mutated cancers. Herein, we report two strategies to access the <sup>18</sup>F-isotopologue of rucaparib by applying a copper-mediated nucleophilic <sup>18</sup>F-fluorodeboronation. The most successful approach features an aldehydic boronic ester precursor that is subjected to reductive amination post-<sup>18</sup>F-labeling and affords [<sup>18</sup>F]rucaparib with an activity yield of 11% ± 3% (<em>n</em> = 3) and a molar activity (<em>A</em><sub>m</sub>) up to 30 GBq/μmol. Preliminary <em>in vitro</em> studies are presented.</p> |
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