Radiosynthesis and preliminary PET evaluation of 18 F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile for imaging AMPA receptors
作者： Gengyang Yuan , Graham B. Jones , Neil Vasdev , Steven H. Liang
DOI: 10.1016/J.BMCL.2016.07.078
关键词:
摘要: To prompt the development of (18)F-labeled positron emission tomography (PET) tracers for α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, we have prepared 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile ([(18)F]8). The radiosynthesis was achieved by a one-pot two-step method that utilized spirocyclic hypervalent iodine(III) mediated radiofluorination to prepare 1-bromo-3-fluorobenzene ([(18)F]15) intermediate with K(18)F. A subsequent copper(I) iodide coupling reaction carried out 2-(2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile (10) [(18)F]8 in 10±2% uncorrected radiochemical yield relative starting (18)F-fluoride >99% purity and 29.6±7.4Gbq/μmol specific activity at time injection. PET imaging studies title radiotracer normal mice demonstrated good brain uptake (peak standardized value (SUV)=2.3±0.1) warrants further vivo validation.
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