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Copper-mediated radiosynthesis of [18F]rucaparib

Abstract:

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 a...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acs.orglett.1c02770

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Role:
Author
ORCID:
0000-0002-0598-7495
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Publisher:
American Chemical Society Publisher's website
Journal:
Organic Letters Journal website
Volume:
23
Issue:
18
Pages:
7290-7294
Publication date:
2021-08-30
Acceptance date:
2021-08-30
DOI:
EISSN:
1523-7052
ISSN:
1523-7060
Pmid:
34459606
Language:
English
Keywords:
Pubs id:
1193504
Local pid:
pubs:1193504
Deposit date:
2021-09-06

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