采用改进的Explora FDG_4模块,基于"两步-两锅"式的放射化学反应处理过程和简便的固相萃取(SPE)方式分离纯化,成功发展了~(18)F-FES的快速、可靠的自动化合成方法.第一步是前体3-O-(甲氧甲基)-16,17-O-磺酰基-16-表雌二醇(MMSE)与活化的~(18)F离子间的亲核放射氟化反应,100℃加热回流反应10 min,生成标记中间体,使用基于硅胶柱的SPE方式分离该标记中间体,除去未反应的起始物.第二步是标记中间体的酸性水解反应,90℃加热反应10 min,生成目标产物~(18)F-FES,使用基于C18和Al_2O_3组成的串联柱的SPE方式分离、纯化所得的~(18)F-FES.总合成时间～70 min,放射化学产率为35%(衰变校正后),放射化学纯度＞95%.%16a-[~(18)F]fluoro-17β-estrogen (~(18)F-FES) is a specific molecular imaging probe of estrogen receptor of breast cancer and has been applied into the clinic diagnosis of breast cancer by PET/CT imaging for the optimization of treatment plan, monitoring of treatment efficiency, improvement of treatment outcome and reduction of treatment cost. A fast, reliable automated synthesis procedure of ~(18)F-FES was developed by modifying a commercial Explora FDG_4 module based on a "two-step, two-pot" radiochemical process and a simple separation way via solid phase extraction (SPE) in this study. In the first step, radiofluorination of precursor 3-O-(methoxymethyl)-16,17-O-sulfuryl-16 -epiestriol and activated ~(18)F ion was carried out at 100℃ for 10 min to form ~(18)F-labeled intermediate, which was separated via SPE based on silica column, so as to remove the non-reacted starting materials. In the second step, acidic hydrolysis of ~(18)F-labeled intermediate was heated at 90℃ for 10 min to produce the target product ~(18)F-FES, which was purified by a serial column consisted of two C18 and one Al_2O_3 cartridges. This newly developed production procedure of ~(18)F-FES could be completed within 70 min with radiochemical yield of about 30% and radiochemical purity of over 95%.
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