Radiochemical synthesis of [18F]fluororaclopride

✍ Scribed by Dale O. Kiesewetter; Thomas Brücke; Ronald D. Finn

• Publisher: Elsevier Science
• Year: 1989
• Weight: 346 KB
• Volume: 40
• Category: Article
• ISSN: 0883-2889
• DOI: 10.1016/0883-2889(89)90126-3

✦ Synopsis

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.