Dzandzi James P K, Vera Denis R Beckford, Valliant John F
Department of Chemistry and Chemical Biology, McMaster University, Hamilton, ON, L8S 4M1, Canada.
J Labelled Comp Radiopharm. 2014 Jul;57(9):551-7. doi: 10.1002/jlcr.3214. Epub 2014 Jul 28.
A new class of fluorous materials was developed to create a hybrid solid-solution phase strategy for the expedient preparation and HPLC-free purification of (125) I-labeled compounds. The system is referred to as a hybrid platform in that it combines solution phase labeling and fluorous solid-phase purification in one step as opposed to two separate individual processes. Treatment of fluorous arylstannanes coated on fluorous silica with [(125) I]NaI and the appropriate oxidant made it possible to produce and selectively isolate the nonfluorous radiolabeled products in high purity (>98%) free from excess starting material and unreacted radioiodine. Examples included simple aryl and heterocyclic (click) derivatives, known radiopharmaceuticals including meta-iodobenzylguanidine (MIBG) and iododeoxyuridine (IUdR), and a new agent with high affinity for prostate-specific membrane antigen. The coated fluorous silica kits are simple to prepare, and reactions can be performed at room temperature using different oxidants generating products in minutes in biocompatible solutions.
开发了一类新型含氟材料，以创建一种混合固溶体相策略，用于快速制备和无高效液相色谱法纯化（125）I标记的化合物。该系统被称为混合平台，因为它将溶液相标记和含氟固相纯化一步结合，而不是两个单独的过程。用[（125）I]NaI和适当的氧化剂处理涂覆在含氟硅胶上的含氟芳基锡烷，使得能够生产并选择性分离出高纯度（>98%）的无氟放射性标记产物，且不含过量的起始原料和未反应的放射性碘。实例包括简单的芳基和杂环（点击）衍生物、已知的放射性药物，包括间碘苄胍（MIBG）和碘脱氧尿苷（IUdR），以及一种对前列腺特异性膜抗原有高亲和力的新型试剂。涂覆的含氟硅胶试剂盒制备简单，反应可在室温下使用不同的氧化剂在生物相容性溶液中几分钟内生成产物。
