title: Radiochemical synthesis of [18F]fluororaclopride.
abstract: The radiochemical synthesis of [18F]Fluororaclopride (S-3,5-dichloro-6-methoxy-N-(1-(2-[18F]fluoroethyl)-2-pyrrolidinylmet hyl) salicylamide) is accomplished via a two step synthesis. [18F]Fluoroethyltriflate is prepared by [18F]fluoride displacement on the bis triflate of ethylene glycol. [18F]Fluoroethyl triflate is then allowed to alkylate a secondary amine precursor to yield [18F]fluororaclopride. Purification of the radiopharmaceutical involves use of a short silica BONDELUT column and subsequent reverse-phase HPLC. The final product is obtained with a radiochemical yield of approximately 15% (corrected for decay) in a synthesis time of approximately 50 min. Fluororaclopride displays a 3- to 4-fold lower affinity for the D2 receptor than does raclopride.
authors.affiliation: Department of Nuclear Medicine, Warren Grant Magnuson Clinical Center, National Institute of Mental Health, Bethesda, MD 20892.
authors.forename: D O
authors.initials: DO
authors.lastname: Kiesewetter
authors.forename: T
authors.initials: T
authors.lastname: Brücke
authors.forename: R D
authors.initials: RD
authors.lastname: Finn
mesh_terms: D005462:Fluorine Radioisotopes; D007553:Isotope Labeling / Q000379:methods*; D011954:Receptors, Dopamine / Q000378:metabolism; D017448:Receptors, Dopamine D2; D012457:Salicylamides / Q000138:chemical synthesis*; D014055:Tomography, Emission-Computed
chemical_list: D005462:Fluorine Radioisotopes; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D012457:Salicylamides; C061342:fluororaclopride