摘要
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15mg 3-N-Boc-5’-O-二甲氧基三苯基-3’-O-nosyl-胸苷溶解在0.5mL DMSO中,使之与18F-在100℃反应5min,之后用1mol/L HCl于110℃下水解5min,用2mol/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30min。产品的放化纯度大于99%,比活度大于740TBq/g(180PBq/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。
3＇-Deoxy-3＇-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 HCl 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 semipreparative HPLC enables us to produce 18F-FLT with a stable yield for clinical use.
出处
《同位素》
CAS
2012年第1期15-20,共6页
Journal of Isotopes
基金
核能开发科技项目资助(2009-1228)
吴阶平医学基金资助(320.6750.08054)
