Efficient Radiosynthesis of 2-[18F]Fluoroadenosine: A New Route to 2-[18F]Fluoropurine Nucleosides

Autor: Franck Sobrio, Fabienne Gourand, Christophe Lorilleux, Martine Dhilly, Louisa Barré, Gwénaëlle Gilbert, Damien Peyronnet, Patrice Marchand
Rok vydání: 2010
Předmět:
Zdroj: ACS Medicinal Chemistry Letters. 1:240-243
ISSN: 1948-5875
DOI: 10.1021/ml100055m
Popis: An efficient method to incorporate the fluorine-18 radionuclide in 2-nitropurine-based nucleosides was developed. The nucleophilic radiofluorination of the labeling precursor with [(18)F]KF under aminopolyether-mediated conditions (Kryptofix 2.2.2/K2CO3) followed by deprotection was straightforward and, after formulation, gave 2-[(18)F]fluoroadenosine, ready for injection with a radiochemical yield of 45 ± 5%, a radiochemical purity of98%, and a specific radioactivity up to 148 GBq/μmol. A micropositron emission tomography imaging and biodistribution study on rodents was reported.
Databáze: OpenAIRE