高产率自动化合成2-^(18)F-2-脱氧-D-葡萄糖  

Efficiently automated synthesis of 2-[^(18)F]-fluoro-2-deoxy-D-glucose

作　　者：唐刚华[1] 唐小兰[2] 王明芳[1] 郭晓君[1] 

机构地区：[1]南方医科大学南方医院核医学科PET中心,广州510515 [2]华南农业大学理学院,广州510642

出　　处：《核技术》2006年第7期531-536,共6页Nuclear Techniques

基　　金：广东省科技计划资助项目(2003C34304);第一军医大学南方医院院长基金资助项目(991015)

摘　　要：研究了2-18F-2-脱氧-D-葡萄糖(18F-FDG)的高产率自动化合成工艺。以三氟甘露糖为前体,采用“一锅法”和TRACERlabFXF-N自动化合成装置,在同一反应瓶中进行亲核氟化、氢氧化钠水解两步反应,然后用小柱中和分离纯化制备了F-FDG注射液。F-FDG的总合成时间约24min,未经校正的放化产率约为60%,1818放化纯度大于99%。采用改进了的自动化工艺合成F-FDG注射液,操作简便,可望成为F-FDG较为实用1818的合成方法。Automated synthetic technology of 2-[18^F]-fluoro-2-deoxy-D-glucose （18^F-FDG） was described. Automated synthesis of 18^F-FDG was performed by ＂one-pot＂ and ＂two-step reaction＂ procedures in TRACERlab FXF-N system. 18^F-FDG injection was obtained via ＂two-step reaction＂ including nucleophilic fluorination of the precursor 1, 3, 4, 6-tetra-O-acetyl-2-O-trifluoromethanesulfony-13-D-mannopyranose with 18^F-fluoride and hydrolysis with NaOH in the same reaction vessel, and subsequently purificated with Sep-Pak cartridges. The uncorrected radiochemical yield of 18^F-FDG was about 60% and radiochemical purity was more than 99% within the total synthesis time about 24 min. Improved synthesis method of 18^F-FDG injection is simple to operate and can become a practical method of preparation.

关 键 词：18^F-FDG 自动化合成 

分 类 号：O615.3[理学—无机化学]