Lim J L, Berridge M S
Department of Radiology, Case Western Reserve University, Cleveland, OH.
Appl Radiat Isot. 1993 Aug;44(8):1085-91. doi: 10.1016/0969-8043(93)90110-v.
An efficient preparation of the hypoxic cell tracer [18F]3-fluoro-1-(2'-nitro-1'-imidazolyl)-2-propanol ([18F]fluoromisonidazole) is reported. This radiopharmaceutical is of interest to probe hypoxic tissue in infarcts and tumors. One-step radiolabeling and rapid protection group removal provided 55-80% yield in 50 min. The process is similar to common fluorine labeling procedures, simplifying the procedure for most laboratories, and offers an improvement over more difficult previous methods. The labeling precursor was prepared in five steps from readily available materials in a straightforward reaction scheme.
报道了一种高效制备缺氧细胞示踪剂[18F]3-氟-1-(2'-硝基-1'-咪唑基)-2-丙醇([18F]氟米索硝唑)的方法。这种放射性药物对于探测梗死灶和肿瘤中的缺氧组织具有重要意义。一步放射性标记和快速去除保护基团在50分钟内可获得55 - 80%的产率。该方法与常见的氟标记程序相似，简化了大多数实验室的操作流程，并且相较于以往更复杂的方法有了改进。标记前体通过五步反应，由容易获得的原料按照简单的反应方案制备而成。
