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

An efficient method to incorporate the fluorine-18 radionuclide in 2-nitropurine-based nucleosides was developed. The nucleophilic radiofluorination of the labeling precursor with [18F]KF under aminopolyether-mediated conditions (Kryptofix 2.2.2/K2CO3) followed by deprotection was straightforward an...

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Published inACS medicinal chemistry letters Vol. 1; no. 6; pp. 240 - 243
Main Authors Marchand, Patrice, Lorilleux, Christophe, Gilbert, Gwénaëlle, Gourand, Fabienne, Sobrio, Franck, Peyronnet, Damien, Dhilly, Martine, Barré, Louisa
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 09.09.2010
Subjects
Letter
2-[18F]fluoroadenosine
PET
nucleoside
purine
[18F]Fluorine
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Summary:An efficient method to incorporate the fluorine-18 radionuclide in 2-nitropurine-based nucleosides was developed. The nucleophilic radiofluorination of the labeling precursor with [18F]KF under aminopolyether-mediated conditions (Kryptofix 2.2.2/K2CO3) followed by deprotection was straightforward and, after formulation, gave 2-[18F]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.
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We thank the Commissariat à l'Energie Atomique for financial support (grant to P.M.).
ISSN:1948-5875
1948-5875
DOI:10.1021/ml100055m