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目的:通过对BAThy前体和BOC前体合成肿瘤增值示踪剂3’-脱氧-3’-[18F]氟胸腺嘧啶(18F-FLT)合成产率的研究,探讨BOC前体在提高18F-FLT合成产率中的价值。方法:联合国内7家PET中心按照国内多中心研究的统一标准进行正电子示踪剂18F-FLT合成研究方面的合作,回旋加速器(MINItrace,GE Healthcare),全自动合成系统(TRACERlab FX F-N;GEHealthcare)。BAThy前体:5’-氧-苯甲酰基-2,3’-胸苷;BOC前体: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]胸腺嘧啶,通过18O(p,n)18F反应生产的18F-离子分别与两种前体进行标记反应并水解,用HPLC进行纯化得到18F-FLT,放化纯度>95%。结果:采用BAThy前体合成18F-FLT,平均合成产率为10.1%。采用BOC前体合成18F-FLT,平均合成产率为23.2%。结论:研究发现BOC前体更容易被18F-离子标记,平均产率比BAThy前体提高了130%。我们还研究了各个因素对于18F-FLT合成的影响,包括碱量与前体量的比、前体的溶剂、水解方式以及操作方法。由于参与的单位分布在国内各个不同的地区,基本能够消除地域因素对合成产率的影响,所得出的结果对于今后的研究有很好的指导意义。
OBJECTIVE: To investigate the synthetic yield of 3’-deoxy-3 ’- [18F] fluorothymidine (18F-FLT) synthesized by BAThy precursors and BOC precursors and to explore the role of BOC precursors in enhancing 18F- The value of FLT synthetic yield. METHODS: Seven PET centers in the United States collaborated on the 18F-FLT synthesis studies of positron tracer according to the uniform standards of multicentre research in China. TRA was developed by GE Healthcare and TRACERlab FX FN; ). BAThy precursor: 5’-O-benzoyl-2,3’-thymidine; BOC precursor: 3-Nt-tert-butoxycarbonyl-1- [5’-O- Oxytrityl) -2’-deoxy-3’-O- (4-nitrophenylsulfonyl) -β-D-threo-pentofuranosyl] thymine was synthesized by 18O (p, n) The 18F-ions produced by the 18F reaction were separately labeled with two precursors and hydrolyzed, and purified by HPLC to obtain 18F-FLT with radiochemical purity> 95%. Results: 18F-FLT was synthesized using BAThy precursor, with an average yield of 10.1%. 18F-FLT was synthesized using BOC precursors with an average yield of 23.2%. Conclusions: The study found that BOC precursors were more easily labeled with 18F-ions and the average yield was 130% higher than BAThy precursors. We also studied the effects of various factors on the 18F-FLT synthesis, including the ratio of base to precursor, solvent, hydrolysis, and method of operation of the precursor. Because the units involved in the distribution in different parts of the country, the basic can eliminate the impact of geographical factors on the yield of synthesis, the results obtained for the future research has a good guiding significance.