O-(2-~(18)F-氟代乙基)-L-酪氨酸的全自动合成

FULLY AUTOMATED SYNTHESIS OF O-(2-~(18)F-FLUOROETHYL)-L-TYROSINE

摘要: 采用PETtrace回旋加速器 FDG全自动合成系统,通过18O(p,n)18F核反应生产18F-,然后与乙二醇二对甲苯磺酸酯发生亲核氟化取代反应,生成2 18F 氟代乙醇对甲苯磺酸酯,后者与L 酪氨酸二钠反应生成O (2 18F 氟代乙基) L 酪氨酸(18F FET)。总合成时间为52min,未校正放化产率约为4%,放化纯度大于95%。

Abstract: 18F- is produced via nuclear reaction 18O(p,n)18F at PET trace Cyclotron. O(218Ffluoroethyl)Ltyrosine(18FFET) is synthesized by a twostep reaction at FDG MicroLab Synthesis. Nucleophilic fluorination reaction of 18Ffluoride with 1,2di(4methyphenylsulfonyloxy)ethane on column give 218F1(4methylphenylsulfonyloxy) ethane, and 18Ffluoroalkylation of Ltyrosine disodium salt with 218F1(4methylsulfonyloxy) ethane formed 18FFET. The overall radiochemical yield with no decay correction is more than 4%, the whole synthesis time is about 52 min, and the radiochemical purity is above 95%. The synthetic 18FFET can be suitable for clinical study with PET imaging.