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既无共沸干燥,也无碱或其他添加剂:一种用于(18)F标记的极简方法。

Neither azeotropic drying, nor base nor other additives: a minimalist approach to (18)F-labeling.

作者信息

Richarz R, Krapf P, Zarrad F, Urusova E A, Neumaier B, Zlatopolskiy B D

机构信息

Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany.

出版信息

Org Biomol Chem. 2014 Oct 28;12(40):8094-9. doi: 10.1039/c4ob01336k.

Abstract

A novel, efficient, time-saving and reliable radiolabeling procedure via nucleophilic substitution with [(18)F]fluoride is described. Different radiolabeled aliphatic and aromatic compounds were prepared in high radiochemical yields simply by heating of quaternary anilinium, diaryliodonium and triarylsulfonium [(18)F]fluorides in suitable solvents. The latter were obtained via direct elution of (18)F(-) from an anion exchange resin with alcoholic solutions of onium precursors. Neither azeotropic evaporation of water, nor a base, nor any other additives like cryptands or crown ethers were necessary. Due to its simplicity this method should be highly suitable for automated radiosyntheses, especially in microfluidic devices.

摘要

描述了一种通过用[¹⁸F]氟化物进行亲核取代的新颖、高效、省时且可靠的放射性标记方法。只需在合适的溶剂中加热季铵盐、二芳基碘鎓盐和三芳基锍盐[¹⁸F]氟化物,就能以高放射化学产率制备不同的放射性标记脂肪族和芳香族化合物。后者是通过用鎓前体的醇溶液从阴离子交换树脂直接洗脱¹⁸F⁻获得的。既不需要水的共沸蒸发,也不需要碱,也不需要任何其他添加剂如穴醚或冠醚。由于其简单性,该方法非常适合自动化放射性合成,特别是在微流控装置中。

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