Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes

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    Abstract

    The polymer supported phosphazene bases PS-P2tBu and the novel PS-P2PEG allowed for efficient extraction of [18F]F− from proton irradiated [18O]H2O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69%) and bromides (42%); the total radiosynthesis time was 35–45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects. The resins could be reused several times with the same or different substrates. The fully automated on-column radiofluorination methodology was applied to the radiosynthesis of the important PET radiotracers [18F]FLT and [18F]FDG. The latter was produced with 40% yield on a 120 GBq scale and passed GMP-regulated quality control required for commercial production of [18F]FDG. The combination of compact form factor, simplicity of [18F]F− recovery and processing, and column reusability can make solid phase radiofluorination an attractive radiochemistry platform for the emerging dose-on-demand instruments for bedside production of PET radiotracers.

    Original languageEnglish
    JournalMolecules
    Volume18
    Issue number9
    Pages (from-to)10531-10547
    ISSN1420-3049
    DOIs
    Publication statusPublished - 2013

    Bibliographical note

    © 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license

    Keywords

    • Chemistry
    • Solid phase radiofluorination
    • Dose-on-demand
    • Polymer-supported phosphazene
    • [18F]
    • Multivariate analysis

    Cite this

    @article{12583b3e3e4443d0a4134f171b5f6344,
    title = "Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes",
    abstract = "The polymer supported phosphazene bases PS-P2tBu and the novel PS-P2PEG allowed for efficient extraction of [18F]F− from proton irradiated [18O]H2O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69{\%}) and bromides (42{\%}); the total radiosynthesis time was 35–45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects. The resins could be reused several times with the same or different substrates. The fully automated on-column radiofluorination methodology was applied to the radiosynthesis of the important PET radiotracers [18F]FLT and [18F]FDG. The latter was produced with 40{\%} yield on a 120 GBq scale and passed GMP-regulated quality control required for commercial production of [18F]FDG. The combination of compact form factor, simplicity of [18F]F− recovery and processing, and column reusability can make solid phase radiofluorination an attractive radiochemistry platform for the emerging dose-on-demand instruments for bedside production of PET radiotracers.",
    keywords = "Chemistry, Solid phase radiofluorination, Dose-on-demand, Polymer-supported phosphazene, [18F], Multivariate analysis",
    author = "Bente Mathiessen and Fedor Zhuravlev",
    note = "{\circledC} 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license",
    year = "2013",
    doi = "10.3390/molecules180910531",
    language = "English",
    volume = "18",
    pages = "10531--10547",
    journal = "Molecules",
    issn = "1420-3049",
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    }

    Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes. / Mathiessen, Bente; Zhuravlev, Fedor.

    In: Molecules, Vol. 18, No. 9, 2013, p. 10531-10547.

    Research output: Contribution to journalJournal articleResearchpeer-review

    TY - JOUR

    T1 - Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes

    AU - Mathiessen, Bente

    AU - Zhuravlev, Fedor

    N1 - © 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license

    PY - 2013

    Y1 - 2013

    N2 - The polymer supported phosphazene bases PS-P2tBu and the novel PS-P2PEG allowed for efficient extraction of [18F]F− from proton irradiated [18O]H2O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69%) and bromides (42%); the total radiosynthesis time was 35–45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects. The resins could be reused several times with the same or different substrates. The fully automated on-column radiofluorination methodology was applied to the radiosynthesis of the important PET radiotracers [18F]FLT and [18F]FDG. The latter was produced with 40% yield on a 120 GBq scale and passed GMP-regulated quality control required for commercial production of [18F]FDG. The combination of compact form factor, simplicity of [18F]F− recovery and processing, and column reusability can make solid phase radiofluorination an attractive radiochemistry platform for the emerging dose-on-demand instruments for bedside production of PET radiotracers.

    AB - The polymer supported phosphazene bases PS-P2tBu and the novel PS-P2PEG allowed for efficient extraction of [18F]F− from proton irradiated [18O]H2O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69%) and bromides (42%); the total radiosynthesis time was 35–45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects. The resins could be reused several times with the same or different substrates. The fully automated on-column radiofluorination methodology was applied to the radiosynthesis of the important PET radiotracers [18F]FLT and [18F]FDG. The latter was produced with 40% yield on a 120 GBq scale and passed GMP-regulated quality control required for commercial production of [18F]FDG. The combination of compact form factor, simplicity of [18F]F− recovery and processing, and column reusability can make solid phase radiofluorination an attractive radiochemistry platform for the emerging dose-on-demand instruments for bedside production of PET radiotracers.

    KW - Chemistry

    KW - Solid phase radiofluorination

    KW - Dose-on-demand

    KW - Polymer-supported phosphazene

    KW - [18F]

    KW - Multivariate analysis

    U2 - 10.3390/molecules180910531

    DO - 10.3390/molecules180910531

    M3 - Journal article

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    SP - 10531

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    JO - Molecules

    JF - Molecules

    SN - 1420-3049

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