PET肿瘤显像剂~(18)F-氟乙基胆碱的自动化合成

18F-氟乙基胆碱(18F-FECH)是反映胆碱代谢的PET肿瘤显像剂,在肿瘤特别是脑肿瘤诊断中显示出良好的应用前景。为了方便临床应用,本工作利用PET-MF-2V-IT-I型18F多功能合成模块,自动化合成18F-FECH。首先18F-与1,2-乙二醇二对甲苯磺酸酯在90℃下发生亲核取代反应,产物未经纯化即与N,N-二甲基乙醇胺在100℃下发生烷基化反应,此后经过C18柱和CM柱进行分离纯化,得到目标产物。整个过程需时约40 min,最终产品放化收率30%(未经时间校正),放化纯度≥99%,室温下可稳定放置6 h。本方法简便易行,合成时间短,收率较高,产品稳定性好,且其它各项指标均符合规定,为临床常规应用提供了保证。

Automatic Synthesis of Tumor Imaging Agent 18F-fluoroethylcholine

18F-fluoroethylcholine（18F-FECH） which reflects the metabolism of choline has been demonstrated to be an promising tumor imaging agent for PET,especially in brain tumor imaging.For utilization in the clinic,this tracer was radiosynthesized automatically with high yields and short synthesis time by using PET-MF-2V-IT-I fluoro-multifunction synthesizer.The two step reactions were processed in the same reaction vessel.The target product was obtained via C18 and CM Sep-pak Plus cartridge with about 30% radiochemical yield（no decay corrected） and more than 99% radiochemical purity within 40 min of total synthesis time,which was stable for 6 h at room temperature.The automatic radiosynthesis procedure have some advantage,such as easy,high yields and short synthesis time and it has potentially utilizable in routine production sites.