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http://dx.doi.org/10.5012/bkcs.2012.33.7.2177

High Yielding [18F]Fluorination Method by Fine Control of the Base  

Lee, Sang-Ju (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine)
Oh, Seung-Jun (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine)
Chi, Dae-Yoon (Department of Chemistry, Sogang University)
Moon, Dae-Hyuk (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine)
Ryu, Jin-Sook (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine)
Publication Information
Bulletin of the Korean Chemical Society / v.33, no.7, 2012 , pp. 2177-2180 More about this Journal
Abstract
New [$^{18}F$]F-fluorination methods using a minimized amount of precursor has been developed by controlling the base concentration. In the first method, pre-conditioning of the anion exchange cartridge with $K_2CO_3$ solution or water was carried out. The trapped [$^{18}F$]fluoride on the cartridge was then eluted by KOMs or KOTf solution. [$^{18}F$]F-Fluorination could be performed without additional base. In the second method, the QMA cartridge was preconditioned with KOMs solutions. Trapped [$^{18}F$]fluoride on the QMA was then eluted with KOMs and additional base, such as KOH, $K_2CO_3$, and $KHCO_3$, was added into the reaction vessel. Method 1 showed a [$^{18}F$]F-incorporation yield of 20.9% for [$^{18}F$]FLT synthesis with 5 mg of precursor. Unlike method 1, a [$^{18}F$]F-incorporation yield of 91.4% was achieved from the same amount of precursor in method 2.
Keywords
[$^{18}F$]Fluoride; [$^{18}F$]Fluorination; KOMs; [$^{18}F$]FLT; Nucleophilic substitution;
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