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无载体添加的4-[¹⁸F]氟碘苯的自动化放射性合成:¹⁸F放射化学中的一种通用构件。

Automated radiosynthesis of no-carrier-added 4-[18F]fluoroiodobenzene: a versatile building block in 18F radiochemistry.

作者信息

Way Jenilee Dawn, Wuest Frank

出版信息

J Labelled Comp Radiopharm. 2014 Feb;57(2):104-9. doi: 10.1002/jlcr.3137.

Abstract

4-[18F]Fluoroiodobenzene ([18F]FIB) is a versatile building block in 18F radiochemistry used in various transition metal-mediated C-C and C-N cross-coupling reactions and [18F]fluoroarylation reactions. Various synthesis routes have been described for the preparation of [18F]FIB. However, to date, no automated synthesis of [18F]FIB has been reported to allow access to larger amounts of [18F]FIB in high radiochemical and chemical purity. Herein, we describe an automated synthesis of no-carrier-added [18F]FIB on a GE TRACERlab™ FX automated synthesis unit starting from commercially available(4-iodophenyl)diphenylsulfonium triflate as the labelling precursor. [18F]FIB was prepared in high radiochemical yields of 89 ± 10% (decay-corrected, n = 7) within 60 min, including HPLC purification. The radiochemical purity exceeded 95%, and specific activity was greater than 40 GBq/μmol. Typically, from an experiment, 6.4 GBq of [18F]FIB could be obtained starting from 10.4 GBq of [18F]fluoride.

摘要

4-[18F]氟碘苯([18F]FIB)是18F放射化学中一种用途广泛的合成砌块,用于各种过渡金属介导的碳-碳和碳-氮交叉偶联反应以及[18F]氟芳基化反应。已经报道了多种制备[18F]FIB的合成路线。然而,迄今为止,尚未有关于[18F]FIB自动合成的报道,以获得大量具有高放射化学纯度和化学纯度的[18F]FIB。在此,我们描述了一种在GE TRACERlab™ FX自动合成装置上,以市售的三氟甲磺酸(4-碘苯基)二苯基锍作为标记前体,自动合成无载体添加的[18F]FIB的方法。在60分钟内,包括高效液相色谱纯化,[18F]FIB的放射化学产率高达89±10%(衰变校正,n = 7)。放射化学纯度超过95%,比活度大于40 GBq/μmol。通常,从一次实验中,以10.4 GBq的[18F]氟化物为起始原料,可以获得6.4 GBq的[18F]FIB。

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