Journal article
Copper-mediated radiosynthesis of [18F]rucaparib
- Abstract:
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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 18F-isotopologue of rucaparib by applying a copper-mediated nucleophilic 18F-fluorodeboronation. The most successful approach features an aldehydic boronic ester precursor that is subjected to reductive amination post-18F-labeling and affords [18F]rucaparib with an activity yield of 11% ± 3% (n = 3) and a molar activity (Am) up to 30 GBq/μmol. Preliminary in vitro studies are presented.
- Publication status:
- Published
- Peer review status:
- Peer reviewed
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- Files:
-
-
(Preview, Accepted manuscript, pdf, 691.4KB, Terms of use)
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- Publisher copy:
- 10.1021/acs.orglett.1c02770
Authors
- Publisher:
- American Chemical Society
- Journal:
- Organic Letters More from this journal
- Volume:
- 23
- Issue:
- 18
- Pages:
- 7290-7294
- Publication date:
- 2021-08-30
- Acceptance date:
- 2021-08-30
- DOI:
- EISSN:
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1523-7052
- ISSN:
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1523-7060
- Pmid:
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34459606
- Language:
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English
- Keywords:
- Pubs id:
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1193504
- Local pid:
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pubs:1193504
- Deposit date:
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2021-09-06
- ARK identifier:
Terms of use
- Copyright holder:
- American Chemical Society
- Copyright date:
- 2021
- Rights statement:
- © 2021 American Chemical Society.
- Notes:
-
This is the accepted manuscript version of the article. The final version is available from American Chemical Society at https://doi.org/10.1021/acs.orglett.1c02770
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