肿瘤乏氧显像剂^(18)F-FAZA的自动化合成

Automated Synthesis of ^(18)F-Labelled FAZA as Hypoxia Imaging Agent

为了制备1--αD-[5’-脱氧-5’-氟阿拉伯呋喃糖基]-2-硝基咪唑(18FAZA),采用两锅法与氟多功能模块,以4~6 mg前体在115℃氟化反应10 min,用C-18柱捕获中间产物,用NaOH水解,HCl中和,进行HPLC分离,得到18FAZA注射液体。总合成时间45 min,放化产率和放射化学纯度分别大于10%与98%。采用两锅法自动合成18F-FAZA,能够满足科研与临床研究的需要。

1-（5-fluoro-5-deoxy-α-D-arabinofuranosyl）-2-nitroimidazole was synthesized by ＂two pot＂ method at a multifunctional CPCU made in China and by using 1-（2,3-di-O-acetyl-5-O-tosyl-α-D-arabinofuranosyl）-2-nitroimidazole as precursor.The precursor（4-6 mg） was fluorinated at 115 ℃ for 10 min.The F-18 labeled intermediate was traped by a C-18 column,then was hydrolyzed using NaOH.The reaction mixture was neutralized by adding HCl,and was purified through HPLC.The pure 18FAZA is obtained for no more than 45 min.The overall radiochemical yield is more than 10%,and the radiopurity is higher than 98%.18FAZA is successfully autosynthesized through ＂two pot＂ method.It can be used in clinical and scientific research.