| Literature DB >> 34459606 |
Zijun Chen1, Gianluca Destro1,2, Florian Guibbal1,2, Chung Ying Chan2, Bart Cornelissen2, Véronique Gouverneur1.
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 activity yield of 11% ± 3% (n = 3) and a molar activity (Am) up to 30 GBq/μmol. Preliminary in vitro studies are presented.Entities:
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Year: 2021 PMID： 34459606 DOI： 10.1021/acs.orglett.1c02770
Source DB: PubMed Journal: Org Lett ISSN： 1523-7052 Impact factor: 6.005