3'-Deoxy-3'-[18F]fluorothymidine (18F-FLT) is a radiotracer for the imaging of tumor proliferation. A clinically applicable automatic system for the preparation of 18F-FLT was developed by modifying a domestic 18F-FDG synthesizer with semipreparative HPLC. Fifteen milligrams of 3-N-Boc-5'-O-dimethoxytrityl-3 '-O-nosyl-thymidine were dissolved in 0. 5 mL DMSO and reacted with dried 18F-fluoride at 100 ℃ for 5 min. The obtained material was hydrolyzed with 1 mol/L HC1 at 110 ℃ for 5 min, and then neutralized with 2 mol/ L NaOH before HPLC purification was performed. The desired radioactive fraction was collected after passing through a 0. 22 m filter into a 30 mL vial as the final product. The 18F-FLT labelling yield was found to be 67. 5% (n = 8) by the radio-TLC method, and 39. 4% (n=6) by the HPLC method. The yield as the final product for clinical use was 21. 2%(n=3, not corrected for decay). The total preparation time, including the time for HPLC purification, was 30 min. The radiochemical purity of the final product was over 99% , and the specific activity was higher than 740 TBq/mg (180 PBq/mol). The final product was stable for more than 6 h in the 10% alcohol solution. This preparation system with semi-preparative HPLC enables us to produce 18F-FLT with a stable yield for clinical use.%采用附接半制备HPLC的国产FDG模块自动化合成了3’-脱氧-3,-[18 F]氟代胸(腺嘧啶脱氧核)苷(18F-FLT).将15 mg 3-N-Boc-5’-O-二甲氧基三苯基-3’-O-nosyl-胸苷溶解在0.5 mL DMSO中,使之与18F在100℃反应5 min,之后用1 mol/L HCl于110℃下水解5 min,用2 mol/L NaOH中和；TLC法测得18F-FLT的标记率为67.5％(n=8),而HPLC测得的标记率为39.4％(n=6)；产品经半制备HPLC分离纯化,最终产品的合成效率为21.2％(n=3,不衰减校正),包括半制备HPLC的分离纯化在内,总的合成时间为30 min.产品的放化纯度大于99％,比活度大于740 TBq/g(180 PBq/mol).产品在10％乙醇中,6h内未见分解.以上结果表明,国产FDG模块配合半制备HPLC,可以合成满足临床需求的18F-FLT.
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