Way Jenilee Dawn, Wuest Frank
J Labelled Comp Radiopharm. 2014 Feb;57(2):104-9. doi: 10.1002/jlcr.3137.
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.
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。
