肿瘤乏氧显像剂<sup>18</sup>F-FAZA的自动化合成

肿瘤乏氧显像剂¹⁸F-FAZA的自动化合成

摘要: 为了制备1-α-D-［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。

Abstract: 1-(5-［¹⁸F］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.