Radiosynthesis of [2-(11)C-carbonyl]dantrolene using [(11)C]phosgene for PET.
Automated radiosynthesis of [2-(11)C-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 [(11)C]phosgene as a labeling agent. After optimization of the automated synthesis conditions and parameters, [2-(11)C-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+/-15.2GBq/micromol at the end of the synthesis.
Takada
Yuuki
Y
Molecular Probe Group, Molecular Imaging Center, National Institute of Radiological Science, Inage-ku, Chiba, Japan.
Ogawa
Masanao
M
Suzuki
Hisashi
H
Fukumura
Toshimitsu
T
D002250:Carbon Radioisotopes / Q000737:chemistry; D003620:Dantrolene / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D010705:Phosgene / Q000737:chemistry*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D010705:Phosgene; D003620:Dantrolene