title: Elimination of contaminant Kryptofix 2.2.2 in the routine production of 2-[18F]fluoro-2-deoxy-D-glucose.
abstract: Radiopharmaceutical solutions of 2-[18F]fluoro-2-deoxy-D-glucose (2-[18F]FDG) prepared via an aminopolyether-supported nucleophilic-substitution mechanism were analyzed for contaminant 4,7,13,16,21,24-hexaoxa-1,10-diazabicyclo-[8,8,8]-hexacosane (Kryptofix 2.2.2). Washing the C18-immobilized [18F]fluoro-tetraacetylated intermediate with 10 mL 0.1 M HCl was found to remove impurity Kryptofix 2.2.2 from the final product. Inclusion of this synthetic step allowed the robotic production of drug-quality 2-[18F]FDG in 52-56% radiochemical yield within 75 min. A thin-layer chromatographic system for the clinical screening of the radiochemical and chemical purity of this radiopharmaceutical is described.
authors.affiliation: Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110.
authors.forename: S M
authors.initials: SM
authors.lastname: Moerlein
authors.forename: J W
authors.initials: JW
authors.lastname: Brodack
authors.forename: B A
authors.initials: BA
authors.lastname: Siegel
authors.forename: M J
authors.initials: MJ
authors.lastname: Welch
mesh_terms: D001643:Bridged Bicyclo Compounds / Q000302:isolation & purification*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds / Q000302:isolation & purification*; D002614:Chelating Agents / Q000302:isolation & purification; D003837:Deoxy Sugars / Q000138:chemical synthesis*; D003847:Deoxyglucose / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000302:isolation & purification; D004340:Drug Contamination; D005462:Fluorine Radioisotopes; D019788:Fluorodeoxyglucose F18; D011854:Radiochemistry
chemical_list: D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds; D002614:Chelating Agents; D003837:Deoxy Sugars; D005462:Fluorine Radioisotopes; D019788:Fluorodeoxyglucose F18; C006071:cryptating agent 222; D003847:Deoxyglucose