81755-10-4Relevant articles and documents
An azeotropic drying-free approach for copper-mediated radiofluorination without addition of base
Zhang, Xiang,Basuli, Falguni,Swenson, Rolf E.
, p. 139 - 145 (2019)
Copper-mediated radiofluorination provides a quick and versatile approach for 18F-labeling of arenes and heteroarenes. However, this method is known to be base sensitive, which has been a barrier for preparative scale radiosynthesis. In this re
Copper-Mediated Radiosynthesis of [18F]Rucaparib
Chen, Zijun,Destro, Gianluca,Guibbal, Florian,Chan, Chung Ying,Cornelissen, Bart,Gouverneur, Véronique
supporting information, p. 7290 - 7294 (2021/09/14)
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.
MCR scaffolds get hotter with 18F-Labeling
Zarganes-Tzitzikas, Tryfon,Clemente, Gon?alo S.,Elsinga, Philip H.,D?mling, Alexander
, (2019/04/16)
Imaging techniques, such as positron emission tomography (PET), represent great progress in the clinical development of drugs and diagnostics. However, the efficient and timely synthesis of appropriately labeled compounds is a largely unsolved problem. Nu
