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

作者：Way Jenilee Dawn; Wuest Frank^*

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2014, 57(2): 104-109.

DOI：10.1002/jlcr.3137

• 4-[F-18]fluoroiodobenzene
• automation
• sulfonium salts
• building block

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

• 出版日期2014-2