title: Aspects of 6-[18F]fluoro-L-DOPA preparation: precursor synthesis, preparative HPLC purification and determination of radiochemical purity.
abstract: A modified method for the synthesis of the intermediate product N-Boc-3,4-di(Boc-O)-6-iodo-L-phenylalanine ethyl ester of the [18F]FDOPA precursor preparation was developed. With the application of bis-(trifluoroacetoxy)-iodobenzene for the iodination step with elemental iodine the yield of the intermediate can be increased from 12% to 50-60%. By replacing silica-gel-based RP HPLC column by a polymer-based column for semi-preparative purification of [18F]FDOPA from the reaction mixture the radiochemical purity of the final product can be increased up to >99%. For the determination of the radiochemical impurity [18F]fluoride a HPLC method using a column with polymer-based RP material was introduced.
authors.affiliation: Institute of Bioorganic and Radiopharmaceutical Chemistry, Forschungszentrum Rossendorf, D-01314, Germany. f.fuechtner@fz-rossendorf.de
authors.forename: F
authors.initials: F
authors.lastname: Füchtner
authors.forename: P
authors.initials: P
authors.lastname: Angelberger
authors.forename: H
authors.initials: H
authors.lastname: Kvaternik
authors.forename: F
authors.initials: F
authors.lastname: Hammerschmidt
authors.forename: B Peric
authors.initials: BP
authors.lastname: Simovc
authors.forename: J
authors.initials: J
authors.lastname: Steinbach
mesh_terms: D002851:Chromatography, High Pressure Liquid; D004295:Dihydroxyphenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000302:isolation & purification*; D008956:Models, Chemical; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000302:isolation & purification; D012680:Sensitivity and Specificity
chemical_list: D019275:Radiopharmaceuticals; C043437:fluorodopa F 18; D004295:Dihydroxyphenylalanine