肿瘤乏氧显像剂^(18)F-FMISO的全自动放射化学合成

Automated Radiochemical Synthesis of ^(18)F-FMISO as Tumor Hypoxia Imaging Agent

采用TRACERlab FXF-N自动化合成装置制备了肿瘤乏氧显像剂18F-FMISO(1-(2’-硝基-1’-咪唑基)-3-[18F]氟-2-丙醇)。以1-(2’-硝基-1’-咪唑基)-2-O-四氢吡喃基-3-O-甲苯磺酸丙二醇为前体,在同一反应瓶中经过亲核氟化、盐酸水解两步反应,然后用HPLC分离纯化系统制备了18F-FMISO。同时还研究了合成中所使用的设备、时间和温度、前体剂量等对合成效率的影响。结果表明,18F-FMISO总合成时间约40 min,未校正18F衰变情况下,放射化学产率约70%,放射化学纯度大于95%。

Automated synthesis of 18F-FMISO（1-（2＇-nitro-1＇-imidazolyl）-3-fluoro-2-propanol） was performed by two-step reaction procedure at TRACERlab FXF-N system.18F-FMISO injection was obtained via two-step reaction including nucleophilic fluorination of the precursor 1-（2＇-nitro-1＇-imidazolyl）-2-O-tetrahydropyranyl-3-O-toluenesulfonylpropanediol with 18F-fluoride and hydrolysis with HCl in the same reaction vessel,and subsequently purificated with HPLC.The influence factors of synthesis yield were investigated.18F-FMISO was performed with the uncorrected radiochemical yield about 70 % and radiochemical purity above 95 % within the total synthesis time about 40 min.