Synthesis of [18F]Fallypride in a Micro-Reactor: Rapid Optimization and Multiple-Production in Small Doses for Micro-PET Studies
Synthesis of [18F]Fallypride in a Micro-Reactor: Rapid Optimization and Multiple-Production in Small Doses for Micro-PET Studies
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DOI：
10.2174/1874471010902010049
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发表时间：
2009-01-01
影响因子：
2.3
通讯作者：
Pike, Victor W.
中科院分区：
文献类型：
--
作者：
Lu, Shuiyu;Giamis, Anthony M.;Pike, Victor W.
商业螺旋管微反应器(NanoTek；Advion)被用作合成小剂量(0.5-1.5MCI)的[F-18]Folypry的便捷平台，用于啮齿类动物脑多巴胺亚型2受体的Micro-PET研究。每次放射合成使用少量(20-40微克；39-77毫摩尔)对甲苯磺酸盐前体和[F-18]氟离子(0.5-2.5毫克)。通过考察前驱物用量、反应温度、流速和[F-18]氟离子与前驱体比例的影响，快速实现了标记反应的优化，[F-18]Folypry的衰变校正放化产率(最高可达88%)重现性好。每一次放射合成中使用的材料数量很少，使得粗品[F-18]FolyPride可以在分析大小的反相高效液相色谱柱上快速纯化，然后再进行静脉注射。通过不断注入试剂前体溶液以获得更大数量的[F-18]FolyPride，很容易实现反应的放大。
A commercial coiled-tube micro-reactor (NanoTek; Advion)was used as a convenient platform for the synthesis of [F-18] fallypride in small doses (0.5-1.5 mCi) for micro-PET studies of brain dopamine subtype-2 receptors in rodents. Each radiosynthesis used low amounts (20-40 mu g; 39-77 nmol) of tosylate precursor and [F-18] fluoride ion (0.5-2.5 mCi). Optimization of the labeling reaction in the apparatus, with respect to the effects of precursor amount, reaction temperature, flow rate and [F-18] fluoride ion to precursor ratio, was achieved rapidly and the decay-corrected radiochemical yield of [F-18] fallypride (up to 88%) was reproducible. The low amounts of material used in each radiosynthesis allowed crude [F-18] fallypride to be purified rapidly on an analytical-size reverse phase HPLC column, preceding formulation for intravenous injection. Scale-up of the reaction was easily achieved by continuously infusing reagent precursor solutions to obtain [F-18] fallypride in much greater quantity.