Abstract
An express method of solid-phase extraction was proposed for the first time for isolation and purification of [18F]flumazenil, a radioligand used to quantify the density of central benzodiazepine receptors by positron emission tomography (PET). This novel approach afforded the radioligand with >97% radiochemical purity and a high chemical purity (nitromazenil content <1 μg mL–1) and considerably reduced the time of the synthesis (from 90 to 50 min). The nonoptimized decay-corrected radiochemical yield was 8%, and the specific radioactivity was >37 GBq μmol–1. The novel synthetic procedure easily can be integrated into automatic modules for the synthesis of clinically used PET radiopharmaceuticals.
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Dedicated to Academician of the Russian Academy of Sciences N. S. Zefirov on the occasion of his 80th birthday.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 3, pp. 0794—0800, March, 2016.
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Nasirzadeh, M., Vaulina, D.D., Kuznetsova, O.F. et al. A novel approach to the synthesis of [18F]flumazenil, a radioligand for PET imaging of central benzodiazepine receptors. Russ Chem Bull 65, 794–800 (2016). https://doi.org/10.1007/s11172-016-1376-1
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DOI: https://doi.org/10.1007/s11172-016-1376-1