乏氧显像剂1-H-1-(3-^(18)F-2-羟基丙基)-2-硝基咪唑的自动化合成  

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

作　　者：唐刚华[1] 王明芳[1] 罗磊[1] 甘满权[1] 

机构地区：[1]南方医科大学南方医院核医学科PET中心,广东广州510515

出　　处：《核化学与放射化学》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)

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.

关 键 词：^18F-FMISO 乏氧显像剂 自动化合成 

分 类 号：O615.3[理学—无机化学]