Improved synthesis of some commonly used PET radioligands by the use of [11C]methyl triflate.
[11C]Methyl triflate was compared with [11C]methyl iodide as a labelled precursor in the synthesis of some commonly used PET radioligands, L-[11C]deprenyl, [11C]m-hydroxyephedrine (MHED), [11C] beta-CIT, [11C] beta-CFT and [11C]SCH 39166 which have been prepared previously in comparatively low yields from [11C]methyl iodide. A new dopamine reuptake radioligand, [11C] alpha-CIT, was also prepared. The results demonstrate that higher yields are obtained with shorter reaction times, lower reaction temperatures and smaller amounts of precursors with [11C]methyl triflate.
Någren
K
K
Turku University Cyclotron/PET Center, Radiopharmaceutical Chemistry Laboratory, Finland.
Müller
L
L
Halldin
C
C
Swahn
C G
CG
Lehikoinen
P
P
D001552:Benzazepines / Q000138:chemical synthesis*; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D003042:Cocaine / Q000031:analogs & derivatives / Q000138:chemical synthesis; D018492:Dopamine Antagonists / Q000138:chemical synthesis; D004809:Ephedrine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D006847:Hydrocarbons, Iodinated; D007202:Indicators and Reagents; D007553:Isotope Labeling / Q000379:methods; D009682:Magnetic Resonance Spectroscopy; D008698:Mesylates; D011869:Radioligand Assay; D012642:Selegiline / Q000138:chemical synthesis*; D014055:Tomography, Emission-Computed / Q000379:methods*
D001552:Benzazepines; D002250:Carbon Radioisotopes; D018492:Dopamine Antagonists; D006847:Hydrocarbons, Iodinated; D007202:Indicators and Reagents; D008698:Mesylates; C058081:ecopipam; D012642:Selegiline; C065363:3-hydroxyephedrine; C078465:methyl triflate; C069723:2beta-carbomethoxy-3beta-(4-iodophenyl)tropane; C014055:methyl iodide; D004809:Ephedrine; D003042:Cocaine