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Preparation of 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) in ionic liquid, [bmim][OTf]
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2006-01-01 , DOI: 10.1002/jlcr.1046
Byung Seok Moon , Kyo Chul Lee , Gwang Il An , Dae Yoon Chi , Seung Dae Yang , Chang Woon Choi , Sang Moo Lim , Kwon Soo Chun

Although 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) is a prospective radiopharmaceutical for the imaging of proliferating tumor cell, it is difficult to prepare large amount of [18F]FLT. We herein describe the preparation of [18F]FLT in an ionic liquid, [bmim][OTf] (1-butyl-3-methyl-imidazolium trifluoromethanesulfonate). At optimized condition, [18F]fluorinationin ionic liquid with 5 µl of 1 M KHCO3 and 5 mg of the precursor yielded 61.5 ± 4.3% (n=10). Total elapsed time was about 70 min including HPLC purification. The rapid synthesis of [18F]FLT can be achieved by removing all evaporation steps. Overall radiochemical yield and radiochemical purity were 30 ± 5% and >95%, respectively. This method can use a small amount of a nitrobenzenesulfonate precursor and can be adapted for automated production. Copyright © 2006 John Wiley & Sons, Ltd.

中文翻译:

在离子液体 [bmim][OTf] 中制备 3'-脱氧-3'-[18F] 氟胸苷 ([18F]FLT)

尽管3'-脱氧-3'-[18F]氟胸苷([18F]FLT)是一种用于增殖肿瘤细胞成像的前瞻性放射性药物,但制备大量[18F]FLT是困难的。我们在此描述了在离子液体 [bmim][OTf](1-丁基-3-甲基-咪唑鎓三氟甲磺酸盐)中制备 [18F] FLT。在优化条件下,[18F] 在离子液体中用 5 μl 1 M KHCO3 和 5 mg 前体氟化产生 61.5 ± 4.3% (n=10)。总经过时间约为 70 分钟,包括 HPLC 纯化。[18F]FLT 的快速合成可以通过去除所有蒸发步骤来实现。总体放射化学产率和放射化学纯度分别为 30±5% 和 >95%。该方法可以使用少量的硝基苯磺酸盐前体,可以适应自动化生产。版权所有 © 2006 John Wiley & Sons,
更新日期:2006-01-01
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