Fast and Easy Drying Method for the Preparation of Activated [ 18 F]Fluoride Using Polymer Cartridge
Fast and Easy Drying Method for the Preparation of Activated [ 18 F]Fluoride Using Polymer Cartridge
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DOI：
10.5012/bkcs.2011.32.1.71
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发表时间：
2011-01
影响因子：
1.7
通讯作者：
J. Seo;B. Lee;Sang Ju Lee;S. Oh;D. Chi
中科院分区：
文献类型：
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作者：
J. Seo;B. Lee;Sang Ju Lee;S. Oh;D. Chi
研究了一种有效的亲核[]试剂，以减少副产物和制备时间。用几种含有惰性有机盐的有机溶液代替传统的水溶液来释放聚合物柱中捕获的[]氟离子和阴离子碱，得出甲醇溶液是最佳选择的结论。与共沸干燥工艺相比，1 min足以完全去除甲醇，通过减少干燥时间，可节省约10%的放射性。用几种阴离子碱对聚合物柱Chromafix（PS-）进行预处理，以取代预加载的碳酸氢盐碱。磷酸盐碱在较低碱度方面显示出比碳酸盐碱更好的结果。叔丁醇溶剂作为反应介质在亲核[18 F]加成反应中起着另一个关键作用，它能抑制消除副产物。在此条件下，反应液的制备速度快，放化产率高（98% Radio-TLC，84%RCY），前体保留率为94%。
An efficient nucleophilic []fluorination has been studied to reduce byproducts and preparation time. Instead of conventional aqueous solution of , several organic solution containing inert organic salts were used to release []fluoride ion and anion bases captured in the polymer cartridge, concluding that methanol solution is the best choice. Comparing to azeotropic drying process, one min was sufficient to remove methanol completely, resulting in about 10% radioactivity saving by reducing drying time. The polymer cartridge, Chromafix (PS-) was pretreated with several anion bases to displace pre-loaded bicarbonate base. Phosphate bases showed better results than carbonate bases in terms of lower basicity. tert-Butanol solvent used as a reaction media played another critical role in nucleophilic [18F]fluorination by suppressing eliminated side product. Consequent []fluorination under the present condition afforded fast preparation of reaction solution and high radiochemical yields (98% radio-TLC, 84% RCY) with 94% of precursor remained.