CAJ | 학술논문

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HCI水解,重复两次后得到产物 18F-FES.结果 18F-FES的合成总时间约80 min,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.
목적 사용자동화합성장치Tracerlab FXFN,제비자격소수체현상제 18F-16α-17β-불자이순(18F-FES).방법　통과량보반응제비 18F-FES:① 18F-화3-O-(갑양갑기)-16,17-O-광선기-16-표자이순발생친핵취대반응;②생성물경HCI수해,중복량차후득도산물 18F-FES.결과 18F-FES적합성총시간약80 min,방화산솔약위10%,방화순도대우95%.결론 정개합성과정자동화완성,조작간편,18F-FES독성소,대인안전,체외교은정,유망성위안전、유효적자격소수체현상제.
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-sulfuryl-16-epiesteriol,then the intermediate is evaporated and hydrolyzed with HCI 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.