雌激素受体显像剂^18F-16α-17β-氟雌二醇的自动化合成

Automated synthesis of the estrogen receptors imaging agent ^18F-FES

目的使用自动化合成装置Tracerlab FXFN，制备雌激素受体显像剂^18F-16α-17β-氟雌二醇（^18F—FES）。方法通过两步反应制备^18F-FES：①^18F和3-O-（甲氧甲基）-16，17-O-磺酰基-16-表雌二醇发生亲核取代反应；②生成物经HCl水解，重复两次后得到产物^18F-FES。结果^18F-FES的合成总时间约80min，放化产率约为10％，放化纯度大于95％。结论整个合成过程自动化完成，操作简便，^18F—FES毒性小，对人安全，体外较稳定，有望成为安全、有效的雌激素受体显像剂。

Objective ^18F-16α-17β-fluoroestradiol （^18F-FES）, an estrogen receptors imaging agent, is synthesized with Tracerlab FXFN system. Methods ^18F-FES is obtained by two steps reactions, including the nucleophilic displacement reaction of no-carrier-added ^18F-fluoride with 3-O-methoxymethyl-16,17-O-suffuryl- 16-epiesteriol, then the intermediate is evaporated and hydrolyzed with HC1 and finally gives ^18F-FES. Results The synthesis of ^18F-FES can be completed in about 80 min. The radiochemical yield and radio-chemical purity are about 10% and 95% respectively. Conclusion The procedure of synthesis is simple and automatical. ^18F- FES has an extremely low toxicity, which suggests that ^18F-FES may be a safe and effective estrogen receptors imaging agent.