Towards automated solid phase radiofluorination for dose-on-demand PET: retention of activity by solid support

    Research output: Contribution to journalJournal articleResearchpeer-review

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    Abstract

    On-column [18F]fluoride trapping and radiofluorination of 2-(naphthalen-1-yl)ethyl-4-methylbenzenesulfonate (C10H7(CH2)2OTs), performed on polystyrene supported phosphazene base PS-PtBu2 yielded [18F]1-(2-fluoroethyl)naphthalene ([18F]C10H7(CH2)2F) in 50% radiochemical yield but left up to 43% of activity unreacted on the resin. This activity could be eluted with Kryptofix/K2CO3 and then used for conventional radiofluorination of the same substrate, suggesting that the column-retained activity was present in the form of [18F]fluoride entrapped in polymer matrix. An approach to minimize the amount of entrapped [18F]fluoride by use of glass beads functionalized with alkylsilane-derivatized phosphazene residues was attempted but was stymied by fluorolysis/hydrolysis of the alkylsilane spacer. The results suggest that the key to high yield of on-column radiofluorination is to minimize the residual [18F]fluoride absorption in the matrix by the judicious choice of solid support.
    Original languageEnglish
    JournalRadiochimica Acta
    Volume103
    Issue number3
    Pages (from-to)227–232
    ISSN0033-8230
    DOIs
    Publication statusPublished - 2015

    Keywords

    • Dose-on-demand PET
    • [18F]
    • Radiofluorination
    • On-column
    • Solid phase

    Cite this

    @article{9e6f54f288cd45ccb5708cb34c787075,
    title = "Towards automated solid phase radiofluorination for dose-on-demand PET: retention of activity by solid support",
    abstract = "On-column [18F]fluoride trapping and radiofluorination of 2-(naphthalen-1-yl)ethyl-4-methylbenzenesulfonate (C10H7(CH2)2OTs), performed on polystyrene supported phosphazene base PS-PtBu2 yielded [18F]1-(2-fluoroethyl)naphthalene ([18F]C10H7(CH2)2F) in 50{\%} radiochemical yield but left up to 43{\%} of activity unreacted on the resin. This activity could be eluted with Kryptofix/K2CO3 and then used for conventional radiofluorination of the same substrate, suggesting that the column-retained activity was present in the form of [18F]fluoride entrapped in polymer matrix. An approach to minimize the amount of entrapped [18F]fluoride by use of glass beads functionalized with alkylsilane-derivatized phosphazene residues was attempted but was stymied by fluorolysis/hydrolysis of the alkylsilane spacer. The results suggest that the key to high yield of on-column radiofluorination is to minimize the residual [18F]fluoride absorption in the matrix by the judicious choice of solid support.",
    keywords = "Dose-on-demand PET, [18F], Radiofluorination, On-column, Solid phase",
    author = "{Ingemann Mathiessen}, Bente and Gregory Severin and Fedor Zhuravlev",
    year = "2015",
    doi = "10.1515/ract-2014-2370",
    language = "English",
    volume = "103",
    pages = "227–232",
    journal = "Radiochimica Acta",
    issn = "0033-8230",
    publisher = "De Gruyter Oldenbourg",
    number = "3",

    }

    Towards automated solid phase radiofluorination for dose-on-demand PET: retention of activity by solid support. / Ingemann Mathiessen, Bente; Severin, Gregory; Zhuravlev, Fedor.

    In: Radiochimica Acta, Vol. 103, No. 3, 2015, p. 227–232.

    Research output: Contribution to journalJournal articleResearchpeer-review

    TY - JOUR

    T1 - Towards automated solid phase radiofluorination for dose-on-demand PET: retention of activity by solid support

    AU - Ingemann Mathiessen, Bente

    AU - Severin, Gregory

    AU - Zhuravlev, Fedor

    PY - 2015

    Y1 - 2015

    N2 - On-column [18F]fluoride trapping and radiofluorination of 2-(naphthalen-1-yl)ethyl-4-methylbenzenesulfonate (C10H7(CH2)2OTs), performed on polystyrene supported phosphazene base PS-PtBu2 yielded [18F]1-(2-fluoroethyl)naphthalene ([18F]C10H7(CH2)2F) in 50% radiochemical yield but left up to 43% of activity unreacted on the resin. This activity could be eluted with Kryptofix/K2CO3 and then used for conventional radiofluorination of the same substrate, suggesting that the column-retained activity was present in the form of [18F]fluoride entrapped in polymer matrix. An approach to minimize the amount of entrapped [18F]fluoride by use of glass beads functionalized with alkylsilane-derivatized phosphazene residues was attempted but was stymied by fluorolysis/hydrolysis of the alkylsilane spacer. The results suggest that the key to high yield of on-column radiofluorination is to minimize the residual [18F]fluoride absorption in the matrix by the judicious choice of solid support.

    AB - On-column [18F]fluoride trapping and radiofluorination of 2-(naphthalen-1-yl)ethyl-4-methylbenzenesulfonate (C10H7(CH2)2OTs), performed on polystyrene supported phosphazene base PS-PtBu2 yielded [18F]1-(2-fluoroethyl)naphthalene ([18F]C10H7(CH2)2F) in 50% radiochemical yield but left up to 43% of activity unreacted on the resin. This activity could be eluted with Kryptofix/K2CO3 and then used for conventional radiofluorination of the same substrate, suggesting that the column-retained activity was present in the form of [18F]fluoride entrapped in polymer matrix. An approach to minimize the amount of entrapped [18F]fluoride by use of glass beads functionalized with alkylsilane-derivatized phosphazene residues was attempted but was stymied by fluorolysis/hydrolysis of the alkylsilane spacer. The results suggest that the key to high yield of on-column radiofluorination is to minimize the residual [18F]fluoride absorption in the matrix by the judicious choice of solid support.

    KW - Dose-on-demand PET

    KW - [18F]

    KW - Radiofluorination

    KW - On-column

    KW - Solid phase

    U2 - 10.1515/ract-2014-2370

    DO - 10.1515/ract-2014-2370

    M3 - Journal article

    VL - 103

    SP - 227

    EP - 232

    JO - Radiochimica Acta

    JF - Radiochimica Acta

    SN - 0033-8230

    IS - 3

    ER -