【作者】 唐刚华； 王明芳； 唐小兰； 罗磊； 甘满权；

【Author】 TANG Gang-hua, WANG Ming-fang, TANG Xiao-lan, LUO Lei, CAN Man-quanPETCenlre, Department of Nuclear Medicine, Nan Fang Hospital, Southern Medical University, Guangzhou 510515, China; College of Science, South China Agricultural University, Guangzhou 510642. China

【机构】 南方医科大学南方医院核医学科PET中心； 华南农业大学理学院；

【摘要】 研究3’-脱氧-3’-18F-氟代胸苷(18F-FLT)自动化合成工艺。采用“一锅法”和TRACERlab FXF-N自动化合成装置,以3-N-t-叔丁氧羰基-1-[5’-O-(4,4’-二甲氧基三苯甲基)-2’-脱氧-3’-O-(4—硝基苯磺酰基)-β-D-苏型-呋喃戊糖基]胸苷为前体,在同一反应瓶中经亲核氟化、盐酸水解两步反应及HPLC分离纯化制备18F-FLT注射液。总合成时间约60 min,未校正放化产率和放化纯度分别大于20%和95%。“一锅法”可用于TRACERlab FXF-N自动化合成装置制备18F-FLT注射液。更多还原

【Abstract】 To study the fully automated synthetic technology of 3’-deoxy-3’-[ F]fluorothymidine ( 18F-FLT). Automated synthesis of 18F-FLTwas performed by one-pot two-step reaction procedure at TRACERlab FXF-N system. 18F-FLT injection was obtained via two-step reaction including nucleophilic fluorination of the precursor molecule3-N-t-butoxycarbonyl-l-[5’-O-(4,4’-dimethoxytriphenylrnethyl)-2’-deoxy-3’-O-(4-nitrobenzenesulfony l)-β-D-threopentofuranosyl]-thymine with 18F-fluoride and subsequent hydrolysis of the protecting group with 1 mol/L HC1 at the same reaction vessel, and by purification with Sep Paks. Fully automated synthesis of 18F-FLT was performed with the uncorrected radiochemical yield above 20% and radiochemical purity above 95% within the total synthesis time about 60 min. Fully automated one-pot synthesis procedure of 18F-FLT injection can be performed at TRACERlab FXF-N system.更多还原