Radiosynthesis of [2-11C-carbonyl]dantrolene using [11C]phosgene for PET

Abstract

Automated radiosynthesis of [2-11C-carbonyl]dantrolene, the substrate of breast cancer resistanceprotein (BCRP/ABCG2), was performed for the first time through a multi-step/one-pot labeling sequencethat started with ethyl 2-{2-[5-(4-nitrophenyl)furfurylidene]hydrazino}acetate and used [11C]phosgeneas a labeling agent. After optimization of the automated synthesis conditions and parameters, [2-11Ccarbonyl]dantrolene was obtained at a radiochemical yield of 34.078.4% (decay-corrected). Theradiochemical purity was greater than 98% and the specific activity was 46.8715.2 GBq/mmol at theend of the synthesis

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