An Efficient Method for Enhancing the Reactivity and Flexibility of [<sup>18</sup>F]Fluoride Towards Nucleophilic Substitution Using Tetraethylammonium Bicarbonate
作者:Laurent Brichard、Franklin I. Aigbirhio
DOI:10.1002/ejoc.201402587
日期:2014.10
standard method used to generate reactive [18F]fluoride for [18F]radiolabelling is to trap it on an anion-exchange cartridge then elute it with a basic aqueous solution, which is then subjected to azeotropic evaporation to remove water. We have now developed a method through the use of tetraethylammonium hydrogen carbonate in which we can obtain efficient recovery of [18F]fluoride (up to 99 %), remove
用于生成用于 [18F] 放射性标记的反应性 [18F] 氟化物的标准方法是将其捕获在阴离子交换柱上,然后用碱性水溶液将其洗脱,然后进行共沸蒸发以除去水。我们现在开发了一种通过使用四乙基碳酸氢铵的方法,在该方法中我们可以获得 [18F] 氟化物的有效回收率(高达 99%),消除对耗时且低效的共沸蒸发过程的要求,并产生反应性 [18F] 氟化物。 18F] 氟化物可以在合成结束时在有水或无水的情况下进行广泛的脂肪族和芳香族 [18F] 亲核取代,放射化学转化率高达 93%。