Kiesewetter D O, Brücke T, Finn R D
Department of Nuclear Medicine, Warren Grant Magnuson Clinical Center, National Institute of Mental Health, Bethesda, MD 20892.
Int J Rad Appl Instrum A. 1989;40(6):455-60. doi: 10.1016/0883-2889(89)90126-3.
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.
[18F]氟哌利多（S-3,5-二氯-6-甲氧基-N-(1-(2-[18F]氟乙基)-2-吡咯烷基甲基)水杨酰胺）的放射化学合成通过两步合成完成。[18F]氟乙基三氟甲磺酸酯是通过在乙二醇双三氟甲磺酸酯上进行[18F]氟化物取代制备的。然后使[18F]氟乙基三氟甲磺酸酯与仲胺前体进行烷基化反应，生成[18F]氟哌利多。放射性药物的纯化包括使用短硅胶BONDELUT柱以及随后的反相高效液相色谱法。最终产物的放射化学产率约为15%（校正衰变），合成时间约为50分钟。氟哌利多对D2受体的亲和力比雷氯必利低3至4倍。
