Literature DB >> 24900201

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

Patrice Marchand1, Christophe Lorilleux1, Gwénaëlle Gilbert1, Fabienne Gourand1, Franck Sobrio1, Damien Peyronnet1, Martine Dhilly1, Louisa Barré1.   

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.

Entities:  

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

Year:  2010        PMID： 24900201      PMCID： PMC4007834          DOI： 10.1021/ml100055m

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  17 in total

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Review 3.  Molecular imaging of cancer with positron emission tomography.

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Review 5.  Adenosine receptors as therapeutic targets.

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6.  Synthesis of 8-[(18)F]fluoroguanine derivatives: in vivo probes for imaging gene expression with positron emission tomography.

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Journal:  Nucl Med Biol       Date:  2000-02       Impact factor: 2.408

7.  Biodistribution and PET imaging of [(18)F]-fluoroadenosine derivatives.

Authors:  Mian M Alauddin; Antranik Shahinian; Ryan Park; Michael Tohme; John D Fissekis; Peter S Conti
Journal:  Nucl Med Biol       Date:  2007-02-22       Impact factor: 2.408

8.  Role of central and peripheral adenosine receptors in the cardiovascular responses to intraperitoneal injections of adenosine A1 and A2A subtype receptor agonists.

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9.  Radiolabeled guanine derivatives for the in vivo mapping of O(6)-alkylguanine-DNA alkyltransferase: 6-(4-[(18)F]Fluoro-benzyloxy)-9H-purin-2-ylamine and 6-(3-[(131)I]Iodo-benzyloxy)-9H-purin-2-ylamine.

Authors:  G Vaidyanathan; D J Affleck; C M Cavazos; S P Johnson; S Shankar; H S Friedman; M O Colvin; M R Zalutsky
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10.  Efficient stereospecific synthesis of no-carrier-added 2-[18F]-fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophilic substitution.

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  3 in total

1.  Fully automated radiosynthesis of 2-[18F]fludarabine for PET imaging of low-grade lymphoma.

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Journal:  Mol Imaging Biol       Date:  2014-02       Impact factor: 3.488

2.  2-[18F]fludarabine, a novel positron emission tomography (PET) tracer for imaging lymphoma: a micro-PET study in murine models.

Authors:  Martine Dhilly; Stéphane Guillouet; Delphine Patin; Fabien Fillesoye; Ahmed Abbas; Fabienne Gourand; Olivier Tirel; Françoise Galateau; Eric T MacKenzie; Charles Dumontet; Michel Leporrier; Louisa Barré
Journal:  Mol Imaging Biol       Date:  2014-02       Impact factor: 3.488

Review 3.  18F-labelled intermediates for radiosynthesis by modular build-up reactions: newer developments.

Authors:  Johannes Ermert
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