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Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes
Hevesy Laboratory, Center for Nuclear Technologies, Technical University of Denmark, Risø Campus, Frederiksborgvej 399, P.O. Box 49, 4000 Roskilde, Denmark
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Received: 24 July 2013; in revised form: 26 August 2013 / Accepted: 27 August 2013 / Published: 30 August 2013
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: solid phase radiofluorination; dose-on-demand; polymer-supported phosphazene; [18F]; multivariate analysis
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MDPI and ACS Style
Mathiessen, B.; Zhuravlev, F. Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes. Molecules 2013, 18, 10531-10547.
Mathiessen B, Zhuravlev F. Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes. Molecules. 2013; 18(9):10531-10547.
Mathiessen, Bente; Zhuravlev, Fedor. 2013. "Automated Solid-Phase Radiofluorination Using Polymer-Supported Phosphazenes." Molecules 18, no. 9: 10531-10547.