The radiosynthesis of [N-methyl-11C]-sertraline.
[N-methyl-11C]Sertraline, a potential agent for the study of the serotonergic system in vivo with positron emission tomography, was prepared by N-methylation of the corresponding norcompound with [11C]iodomethane, which was itself prepared from cyclotron-produced [11C]carbon dioxide. Under the best conditions found [norsertraline free base (20 mM) in DMF (0.70 mL), 120 degrees C for 8 min] [N-methyl-11C]-sertraline can be prepared in 43% radiochemical yield from [11C]iodomethane (decay-corrected), corresponding to 20% overall radiochemical yield from [11C]carbon dioxide (decay-corrected), with high specific radioactivity. Preparations can be ready for i.v. injection 50 min from the end of radionuclide production.
Lasne
M C
MC
MRC Cyclotron Unit, Hammersmith Hospital, London, U.K.
Pike
V W
VW
Turton
D R
DR
D015057:1-Naphthylamine / Q000031:analogs & derivatives; D002250:Carbon Radioisotopes; D007553:Isotope Labeling / Q000379:methods*; D009281:Naphthalenes / Q000031:analogs & derivatives; D012702:Serotonin Antagonists; D020280:Sertraline; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D009281:Naphthalenes; D012702:Serotonin Antagonists; D015057:1-Naphthylamine; D020280:Sertraline