简便、快速自动化合成肿瘤显像剂^(18)F-氟代乙酸盐和1-H-1-(3-^(18)F-2-羟基丙基)-2-^(18)F-硝基咪唑  

Simple and rapid synthesis of tumor imaging agents^(18)F-FAC and ^(18)F- FMISO

作　　者：唐刚华[1] 唐小兰[2] 王明芳[1] 罗磊[1] 甘满权[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8期581-586,共6页Nuclear Techniques

基　　金：广东省科技计划资助项目(2003C34304)

摘　　要：用“一锅法”和TRACERlab FXF-N自动化合成仪系统合成了18F-氟代乙酸盐(18F-FAC)和1-H-1-(3-18F-2-羟基丙基)-2-硝基咪唑(18F-FMISO)。以溴代乙酸苄酯为前体,在同一反应瓶中经亲核氟化、NaOH水解两步反应及Sep Pak小柱分离纯化制备了18F-FAC注射液,总合成时间小于40min,未经校正的放化产率和放化纯度分别大于45％和99％。以1-(2’-硝基-1’-咪唑基)-2-O-四氢吡喃基-3-O-甲苯磺酰基丙二醇为原料,用类似方法制备了18F-FMISO注射液,总合成时间小于40 min,未经校正的放化产率和放化纯度分别大于40％和95％。采用“一锅法”自动化合成18F-FAC和18F-FMISO注射液,操作简便,该工艺可用制备2-18F-2-脱氧-D-葡萄糖(18F-FDG)的全自动化合成模块来制备18F-FAC和18F-FMISO注射液。The fully automated synthesis of tumor imaging agents ^18F-fluoroacetate （^18F-FAC） and 1-H-1-（3-[^18F]fluoro-2-hydro-xylpropyl）-2-nitroimidazole （^18F-FMISO） via ＂one-pot＂ procedure in TRACERlab FXF-N synthesizer is described. ^18F-FAC injection was prepared via two-step reactions including nucleophilic fluorination of the precursor benzyl bromoacetate with ^18F-fluoride and subsequently hydrolysis with NaOH at the same reaction vessel, and purified with Sep Pak cartridges. The uncorrected radiochemical yield of ^18F-FAC was about 45%, the radiochemical purity was more than 99%, and the whole synthesis time was less than 40 min. ^18F-FMISO injection was prepared by the similar method. The uncorrected radiochemical yield of ^18F-FMISO is above 40%, the radiochemical purity is above 95%, and the total synthesis time was less than 40 min. The fully automated one-pot synthesis procedures of ^18F-FAC and ^18F-FMISO injection are easy to operate and can be performed in any automated system designed for the synthesis of 2-^18F-2-deoxy-D-glucose （^18F-FDG） by the nucleophilic substitution.

关 键 词：^18F-氟代乙酸盐 ^18F-FMISO 肿瘤显像剂 乏氧显像剂 自动化合成 

分 类 号：R817.4[医药卫生—影像医学与核医学] R91[医药卫生—放射医学]