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

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40 min,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40min,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.

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

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.