Efficient radiosynthesis of 2-[(18)f]fluoroadenosine: a new route to 2-[(18)f]fluoropurine nucleosides

ACS Med Chem Lett. 2010 May 28;1(6):240-3. doi: 10.1021/ml100055m. eCollection 2010 Sep 9.

Abstract

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 of >98%, and a specific radioactivity up to 148 GBq/μmol. A micropositron emission tomography imaging and biodistribution study on rodents was reported.

Keywords: 2-[18F]fluoroadenosine; PET; [18F]Fluorine; nucleoside; purine.