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

被引：12
|
作者：
Marchand, Patrice [1 ]
Lorilleux, Christophe [1 ]
Gilbert, Gwenaelle [1 ]
Gourand, Fabienne [1 ]
Sobrio, Franck [1 ]
Peyronnet, Damien [1 ]
Dhilly, Martine [1 ]
Barre, Louisa [1 ]
机构：
[1] Univ Caen Basso Normandie, CI NAPS UMR 6232, Lab Dev Methodol Tomog Emiss Positons, CEA DSV 12BM, Caen, France
来源：
ACS MEDICINAL CHEMISTRY LETTERS | 2010年 / 1卷 / 06期
关键词：
F-18]Fluorine; nucleoside; purine; 2-[F-18]fluoroadenosine; PET; POSITRON-EMISSION-TOMOGRAPHY; ADENOSINE RECEPTORS; GENE-EXPRESSION; PET; DERIVATIVES; PROBES; PURINE;
D O I：
10.1021/ml100055m
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
An efficient method to incorporate the fluorine-18 radionuclide in 2-nitropurine-based nucleosides was developed. The nucleophilic radiofluorination of the labeling precursor with [F-18]KF under aminopolyether-mediated conditions (Kryptofix 2.2.2/K2CO3) followed by deprotection was straightforward and, after formulation, gave 2-[F-18]fluoroadenosine, ready for injection with a radiochemical yield of 45 +/- 5%, a radiochemical purity of >98%, and a specific radioactivity up to 148 GBq/mu mol. A micropositron emission tomography imaging and biodistribution study on rodents was reported.
引用
收藏
页码：240 / 243
页数：4
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