Takahashi Toshihiro, Mizuno Takashi, Ido Tatsuo, Iwata Ren, Watanabe Ken-ichi
Radioisotope Center, Niigata University, Asahimachi-dori 1-757, Niigata 951-8510, Japan.
Appl Radiat Isot. 2003 May;58(5):557-66. doi: 10.1016/s0969-8043(03)00053-8.
For preparing [18F]labeled compounds free from bromo-compounds for PET (positron emission tomography) studies, we propose the following two processes in which no separation is needed between the fluoro-compound and bromo-compound : (1). the bromo-compound is first converted into O-tosylate, which is then [18F]fluorinated; and (2). after [18F]fluorination of the bromo-compound, its excess is converted into an easily separable compound, e.g., phthalimide-compound. Direct tosylation with silver tosylate was effected in 65-85% yield for most commercial bromo-compounds, and with potassium phthalimide, the bromo-compounds in cold run were converted easily into phthalimide-compounds in 84-90% yield.
为制备用于正电子发射断层扫描（PET）研究的不含溴化合物的[18F]标记化合物，我们提出以下两种无需在氟化合物和溴化合物之间进行分离的方法：（1）. 首先将溴化合物转化为邻甲苯磺酸酯，然后进行[18F]氟化；（2）. 在溴化合物进行[18F]氟化后，将其过量部分转化为易于分离的化合物，例如邻苯二甲酰亚胺化合物。对于大多数市售溴化合物，用对甲苯磺酸银直接进行甲苯磺酰化的产率为65 - 85%，而使用邻苯二甲酰亚胺钾时，冷反应中的溴化合物很容易转化为邻苯二甲酰亚胺化合物，产率为84 - 90%。
