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
相关论文
共 50 条
  • [1] Synthesis of 2-[18F]fluoroadenosine (2-[18F]FAD) as potential radiotracer for studying malignancies by PET
    Horti, Andrew G.
    Ravert, Hayden T.
    Mathews, William B.
    Abraham, Edward H.
    Wahl, Richard L.
    Dannals, Robert F.
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2006, 49 (09): : 811 - 815
  • [2] Radiosynthesis and in vitro evaluation of 2-(2-[18F]fluoroethyl)-L-phenylalanine (2-[18F]FELP) as a new tumor tracer for PET.
    Kersemans, Ken
    Bauwens, Matthias
    Mertens, John
    De Vos, Filip
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2013, 56 : S368 - S368
  • [3] Fully Automated Radiosynthesis of 1-(2-[18F]Fluoroethyl)-LTryptophan ([18F]FETrp)
    Jiang, Huailei
    Guo, Yan
    Cai, Hancheng
    Viola, Nerissa
    Shields, Anthony
    Muzik, Otto
    Juhasz, Csaba
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2023, 126 : S63 - S63
  • [4] Efficient preparation of 2-[18F] fluorophenylalanine (2-[18F] FPhe) by Cu-mediated radiofluorination
    Modemann, D.
    Zlatopolskiy, B.
    Ermert, J.
    Neumaier, B.
    [J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2017, 44 : S347 - S347
  • [5] Copper-mediated reduction of 2-[18F]fluoroethyl azide to 2-[18F]fluoroethylamine
    Glaser, Matthias
    Arstad, Erik
    Gaeta, Alessandra
    Nairne, James
    Trigg, William
    Robins, Edward G.
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2012, 55 (09): : 326 - 331
  • [6] Cu/H+ mediated Reduction of 2-[18F]Fluoroethylazide to 2-[18F]Fluoroethylamine
    Glaser, Matthias
    Arstad, Erik
    Gaeta, Alessandra
    Woodcraft, John
    Nairne, James
    Trigg, William
    Robins, Edward
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2011, 54 : S464 - S464
  • [7] Radiosynthesis of 2-[18F]fluoro-4-borono-phenylaranine ([18F]FBPA) using copper mediated oxidative aromatic nucleophilic [18F]fluorination.
    Honda, Natsuki
    Yoshimoto, Mitsuki
    Mizukawa, Yosuke
    Osaki, Katsuhiko
    Kanai, Yasukazu
    Kurihara, Hiroaki
    Tateishi, Hiroyuki
    Takahashi, Kazuhiro
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2017, 60 : S512 - S512
  • [8] One step radiosynthesis of 4-nitrophenyl 2-[18F]fluoropropionate ([18F]NFP): Simplified automated preparation of the αVβ3 integrin imaging agents [18F]GalactoRGD and [18F]-FPPRGD2
    Haskali, Mohammad
    Roselt, Peter
    Karas, John
    Denoyer, Delphine
    Noonan, Wayne
    Wichmann, Christian
    Katsifis, Andrew
    Hicks, Rodney
    Hutton, Craig
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2013, 56 : S123 - S123
  • [9] Radiosynthesis of 3-(2′-[18F]fluoro)-flumazenil ([18F]FFMZ)
    Wadsak, W
    Mitterhauser, M
    Mien, LK
    Tögel, S
    Keppler, B
    Dudczak, R
    Kletter, K
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2003, 46 (13): : 1229 - 1240
  • [10] Radiosynthesis of [18F]fluoromethyl tosylate for [18F]fluoromethylation
    Friederike, Beyerlein
    Markus, Piel
    Tobias, Ross L.
    Frank, Roech
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2011, 54 : S483 - S483
12345