肿瘤显像剂^(18)F-氟代乙酸盐的自动化合成

Automated synthesis of ^(18)F-fluoroacetate as tumor imaging agent

为研究肿瘤显像剂18F-氟代乙酸盐(18F-FAC)的自动化合成工艺,采用“一锅法”和TRACERlabFXF-N自动化合成装置,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HPLC系统分离纯化制备18F-FAC注射液。总合成时间约50min,未校正放化产率和放化纯度分别大于45%和99%。采用“一锅法”自动化合成18F-FAC,操作简便,能满足科研和临床正电子发射断层显像的需要。

To improve the automated synthesis technology of ^18F-fluoroacetate （^18F-FAC） as tumor imaging agent, the one-pot procedure at TRACERlab FXF-N module was tried. ^18F-FAC injection was obtained via a two-step reaction including nucleophilic fluorination of the precursor benzyl bromoacetate with ^18F-fluoride and subsequent hydrolysis of the protecting group with 3 mol/L NaOH at the same reaction vessel, and purification with HPLC system, ^18F-FAC was automatically synthesized with an uncorrected radiochemical yield of more than 45% and radiochemical purity of more than 99% in the synthesis process of about 50 min. ^18F-FAC injection is easy to be obtained and can be used for clinical and scientific study with positron emission tomography （PET） imaging.