摘要
采用改进的Explora FDG4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18F-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18F离子间的亲核放射氟化反应,100℃加热回流反应10min,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10min,生成目标产物18F-FES,使用基于C18和Al2O3组成的串联柱的SPE方式分离、纯化所得的18F-FES。总合成时间～70min,放射化学产率为35%(衰变校正后),放射化学纯度>95%。
16α-[^18F]fluoro-17β-estrogen （^18F-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 ^18F-FES was developed by modifying a commercial Explora FDG4 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 ^18F ion was carded out at 100℃ for 10 rain to form ^18F-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 ^18F-labeled intermediate was heated at 90℃ for 10 min to produce the target product ^18F-FES, which was purified by a serial column consisted of two C18 and one Al2O3 cartridges. This newly developed production procedure of ^18F-FES could be completed within 70 min with radiochemical yield of about 30% and radiochemical purity of over 95 %.
出处
《核技术》
CAS
CSCD
北大核心
2009年第11期839-844,共6页
Nuclear Techniques
基金
国家自然科学基金(30700188)
上海市卫生局青年科研项目(2006Y11)资助
