肿瘤显像剂^(18)F-FLT的化学合成效率的影响因素

Influence Factor on Synthesis Yield of ^(18)F-FLT as Tumor Imaging Agent

为提高^(18)F-FLT合成效率,研究以N-BOC为前体,采用"一锅法"和TRACERlab FXF-N自动化合成^(18)FFLT时各种因素对合成效率的影响。结果显示,前体的化学量和合成体系中水的残留明显影响^(18)F-FLT的合成效率。增加N-BOC前体量,可明显提高合成效率;体系中残留水的存在明显降低合成效率;75、90与105℃的酸水解温度对合成效率无明显影响;K222与K2CO3的物质的量比为2.5时,^(18)F-FLT的合成效率最大。以上结果提示,使用TRACERlab FXF-N多功能模块,通过优化合成参数,可明显提高^(18)F-FLT的合成效率,提高放化纯度和化学纯度。

3’-deoxy-3’-[18F]fluorothymidine（18F-FLT） was prepared from N-BOC precursor to improve the synthesis yield,chemical purity and radiochemical purity of18F-FLT by TRACERlab FXF-N system. Automated synthesis of18F-FLT was performed by one-pot two-step reaction procedure at TRACERlab FXF-N system. The results showed that residual water in synthesis system and the amount of precursor could affect the synthesis yield dramatically. When The amount of precursor increased,the synthesis yield of N-BOC was higher. The residual water could decrease the synthesis yield. Hydrolysis temperature had no significant effect on the synthesis efficiency.The molar ratio of K222 and K2CO3was 2. 5,18F-FLT synthesis efficiency was the highest. The high chemical purity,radiochemical purity and synthesis yield could be obtained by optimizing the parameter of synthesis with TRACERlab FXF-N system.