Reactivity of electrochemically concentrated anhydrous [ 18F]fluoride for microfluidic radiosynthesis of 18F-labeled compounds

In order to demonstrate the usefulness of electrochemically concentrated [ 18F]fluoride the reactivity of the [K +/K.222] 18F − complex concentrated in an aprotic solvent (ca. 60 μL) was evaluated via nucleophilic 18F-substitution reactions through radiosynthesis of [ 18F]FDG, [ 18F]FMISO, [ 18F]flu...

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Bibliographic Details
Published in:Applied radiation and isotopes 2012, Vol.70 (1), p.193-199
Main Authors: Wong, Rebecca, Iwata, Ren, Saiki, Hidekazu, Furumoto, Shozo, Ishikawa, Yoichi, Ozeki, Eiichi
Format: Article
Language:English
Subjects:
[ 18F]fluoride
Electrochemistry - instrumentation
Equipment Design
Equipment Failure Analysis
F-18
Fluorine Radioisotopes - chemistry
Isotope Labeling - instrumentation
Microfluidic Analytical Techniques - instrumentation
Microfluidics
PET probe
Radiosynthesis
Water - chemistry
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Summary:In order to demonstrate the usefulness of electrochemically concentrated [ 18F]fluoride the reactivity of the [K +/K.222] 18F − complex concentrated in an aprotic solvent (ca. 60 μL) was evaluated via nucleophilic 18F-substitution reactions through radiosynthesis of [ 18F]FDG, [ 18F]FMISO, [ 18F]flumazenil and [ 18F]fluoromethyl bromide. The substitutions were carried out in a microfluidic reaction flow cell and the effects of reaction time, temperature, precursor concentration and reaction solvent on the 18F-substitution yields were investigated. The 18F-fluorination yields for the four 18F-labeled compounds under optimized conditions (98% for protected [ 18F]FDG, 80% for protected [ 18F]FMISO, 20% for [ 18F]flumazenil and 60% for [ 18F]fluoromethyl bromide) were comparable to or higher than those obtained by conventional means. In this study it is clearly demonstrated that electrochemically concentrated [ 18F]fluoride enables microfluidic radiosynthesis by effectively reducing synthesis times and especially by increasing radiochemical yields of products labile at high temperatures. ► The high reactivity of electrochemically concentrated [ 18F]fluoride was shown. ► Microfluidic radiosynthesis with the [ 18F]fluoride effectively reduced synthesis time. ► Microfluidic radiosynthesis increased yields of products labile at high temperatures.
ISSN:0969-8043
1872-9800
DOI:10.1016/j.apradiso.2011.09.022