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• W2736722163 abstract "Positron emission tomography (PET) is an important molecular imaging technique for medical diagnosis, biomedical research and drug development. PET tracers for molecular imaging contain β+-emitting radionuclides, such as carbon-11 (t1/2 = 20.4 min) or fluorine-18 (t1/2 = 109.8 min). The [18F]2-fluoro-pyridyl moiety features in a few prominent PET radiotracers, not least because this moiety is usually resistant to unwanted radiodefluorination in vivo. Various methods have been developed for labeling these radiotracers from cyclotron-produced no-carrier-added [18F]fluoride ion, mainly based on substitution of a leaving group, such as halide (Cl or Br), or preferably a better leaving group, such as nitro or trimethylammonium. However, precursors with a good leaving group are sometimes more challenging or lengthy to prepare. Methods for enhancing the reactivity of more readily accessible 2-halopyridyl precursors are therefore desirable, especially for early radiotracer screening programs that may require the quick labeling of several homologous radiotracer candidates. In this work, we explored a wide range of additives for beneficial effect on nucleophilic substitution by [18F]fluoride ion in 5-subsituted 2-halopyridines (halo = Cl or Br). The nucleophilic cyclic tertiary amines, quinuclidine and DABCO, proved effective for increasing yields to practically useful levels (> 15%). Quinuclidine and DABCO likely promote radiofluorination through reversible formation of quaternary ammonium intermediates." @default.
• W2736722163 created "2017-07-31" @default.
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• W2736722163 date "2017-09-04" @default.
• W2736722163 modified "2023-10-05" @default.
• W2736722163 title "Quinuclidine and DABCO Enhance the Radiofluorination of 5-Substituted 2-Halopyridines" @default.
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• W2736722163 doi "https://doi.org/10.1002/ejoc.201700970" @default.
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