摘要
为了制备1 H 1 (3 18F 2 羟基丙基) 2 18F 硝基咪唑(18 F FMISO),采用“一锅法”和 Tracerlab FXF N自动化合成装置,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,经亲核氟化、水解两步反应制备18F FMISO注射液。总合成时间小于60 min,放化产率和放化纯度分别大于 60%和 99%。采用“一锅法”自动化合成18F FMISO,操作简便,能满足科研和临床正电子发射断层显像的需要。
1-H-1-(3-[18F]-fluoro-2-hydroxylpropyl)-2-nitroimidazole (18F-FMISO) is synthesized by one pot method at Tracerlab FXF-N system. By using 1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonyl - propanediol as the precursor, 18F-FMISO is obtained via two-step reactions, including the nucleophilic fluoration of the precursor to yield an intermediate 1-(2'-nitro-1'-imid-azolyl)-2-O-tetrahydropyranyl)-3-[18F] - fluoropropanol, and the acidic hydrolysis of the intermediate. The procedure is simple and can be completed within 60 min. The radiochemical yield and radio-chemical purity are higher than 60% and 99%, respectively. Toxicological assays indicate that the final product is bacteria-free and non-toxic, and meets the requirements for radiopharmacy. It can be used in clinical and scientific research.
出处
《核化学与放射化学》
EI
CAS
CSCD
北大核心
2005年第1期43-46,64,共5页
Journal of Nuclear and Radiochemistry
基金
广东省科技计划资助项目(2003C34304)
第一军医大学南方医院院长基金资助项目(991015)
