Radiosynthesis and preliminary PET evaluation of 18F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile for imaging AMPA receptors

Add time:09/04/2019    Source:sciencedirect.com

To prompt the development of 18F-labeled positron emission tomography (PET) tracers for the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, we have prepared 18F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile ([18F]8). The radiosynthesis was achieved by a one-pot two-step method that utilized a spirocyclic hypervalent iodine(III) mediated radiofluorination to prepare the 18F-labeled 1-bromo-3-fluorobenzene ([18F]15) intermediate with K18F. A subsequent copper(I) iodide mediated coupling reaction was carried out with 2-(2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile (10) to [18F]8 in 10 ± 2% uncorrected radiochemical yield relative to starting 18F-fluoride with >99% radiochemical purity and 29.6 ± 7.4 Gbq/μmol specific activity at the time of injection. PET imaging studies with the title radiotracer in normal mice demonstrated good brain uptake (peak standardized uptake value (SUV) = 2.3 ± 0.1) and warrants further in vivo validation.

We also recommend Trading Suppliers and Manufacturers of 2-HYDROXY-4-METHYL-BENZONITRILE (cas 18495-14-2). Pls Click Website Link as below: cas 18495-14-2 suppliers

Prev:Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor
Next:Technical NoteSynthesis of a carbon-14 analogue of 8-chloro-11-(4-methyl-1-piperazinyl)-11-[14C]-dibenz[b,f][1,4]oxazepine)