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Copper-Mediated Radiosynthesis of [18F]Rucaparib.
Zijun Chen1, Gianluca Destro1,2, Florian Guibbal1,2
1Chemistry Research Laboratory, Oxford University, Oxford OX1 3TA, U.K.
Organic Letters
|August 30, 2021
Summary
Researchers developed a new method to create a radioactive version of the cancer drug rucaparib, called [18F]rucaparib. This radiolabeled compound is crucial for advanced imaging in BRCA-mutated cancer diagnostics.
Area of Science:
- Radiochemistry
- Organic Synthesis
- Medical Imaging
Background:
- Rucaparib is a PARP inhibitor used for BRCA-mutated cancers.
- Development of radiolabeled analogs is essential for diagnostic imaging.
- Fluorine-18 (18F) labeling enables positron emission tomography (PET) imaging.
Purpose of the Study:
- To synthesize the 18F-isotopologue of rucaparib, [18F]rucaparib.
- To evaluate copper-mediated nucleophilic 18F-fluorodeboronation strategies.
- To assess the potential of [18F]rucaparib for in vitro studies.
Main Methods:
- Two strategies for 18F-labeling of rucaparib were explored.
- Copper-mediated nucleophilic 18F-fluorodeboronation was applied.
- An aldehydic boronic ester precursor was used for reductive amination post-labeling.
Main Results:
- The most successful method yielded [18F]rucaparib with an 11% ± 3% activity yield.
- Molar activity (Am) reached up to 30 GBq/micromol.
- Preliminary in vitro data were obtained.
Conclusions:
- A viable synthetic route to [18F]rucaparib was established.
- The developed method shows promise for producing PET imaging agents.
- Further in vitro and in vivo studies are warranted.
