3’-脱氧-3’-^(18)F-氟代胸腺嘧啶核苷的合成研究  

Synthesis of 3'-deoxy-3'-[^(18)F] fluorothymidine

作　　者：范文博[1] 彭添兴[1] 颜和平[1] 

机构地区：[1]福建医科大学附属厦门第一医院核医学科PET中心,福建厦门361003

出　　处：《应用化工》2008年第1期80-82,共3页Applied Chemical Industry

摘　　要：采用TRACERlab FXF-N自动化合成装置制备了肿瘤显像剂3’-脱氧-3’-18F-氟代胸腺嘧啶核苷(18F-FLT)。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,经过亲核氟化、盐酸水解两步反应及HPLC分离纯化制备18F-FLT,研究了不同因素对合成效率的影响。结果表明,总合成时间约55 min,未校正18F衰变情况下,放射化学产率约25%,放化纯度大于95%。Automated synthesis of 3＇ -deoxy-3 ＇ -[^18F ] fluorothymidine （^18F-FLT） was performed by two-step reaction procedure at TRACERlab FXF-N system. ^18F-FLT was obtained via two-step reaction including nucleophilic fluorination of the precursor molecule3-N-t-butoxycarbonyl-1-[5＇-O-（4,4＇ -dimethoxy triphenylmethyl）-2＇-deoxy-3 ＇-O-（4-nitrobenzenesulfonyl）-β-D-threopentofuranosyl]-thymine with ^18F-fluoride and subsequent hydrolysis of the protecting group with HCl at the same reaction vessel,and by purification with Sep Paks. The influence factors on synthesis yield were investigated. ^18F-FLT was performed with the uncorrected radiochemical yield above 25% and radiochemical purity above 95% within the total synthesis time about 55 min.

关 键 词：肿瘤显像剂 化学合成 ^18F—FLT 自动化 

分 类 号：TQ426[化学工程]