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

Automated radiosynthesis of [2-11C-carbonyl]dantrolene, the substrate of breast cancer resistance protein (BCRP/ABCG2), was performed for the first time through a multi-step/one-pot labeling sequence that started with ethyl 2-{2-[5-(4-nitrophenyl)furfurylidene]hydrazino}acetate and used [11C]phosgene as a labeling agent. After optimization of the automated synthesis conditions and parameters, [2-11C-carbonyl]dantrolene was obtained at a radiochemical yield of 34.0±8.4% (decay-corrected). The radiochemical purity was greater than 98% and the specific activity was 46.8±15.2 GBq/μmol at the end of the synthesis.