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Automated radiosynthesis of no‐carrier‐added 4‐[ 18 F]fluoroiodobenzene: a versatile building block in 18 F radiochemistry
Author(s) -
Way Jenilee Dawn,
Wuest Frank
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3137
Subject(s) - chemistry , radiosynthesis , radiochemistry , trifluoromethanesulfonate , block (permutation group theory) , yield (engineering) , specific activity , nuclear chemistry , organic chemistry , catalysis , materials science , mathematics , in vivo , biology , enzyme , metallurgy , geometry , microbiology and biotechnology
4‐[ 18 F]Fluoroiodobenzene ([ 18 F]FIB) is a versatile building block in 18 F radiochemistry used in various transition metal‐mediated C–C and C–N cross‐coupling reactions and [ 18 F]fluoroarylation reactions. Various synthesis routes have been described for the preparation of [ 18 F]FIB. However, to date, no automated synthesis of [ 18 F]FIB has been reported to allow access to larger amounts of [ 18 F]FIB in high radiochemical and chemical purity. Herein, we describe an automated synthesis of no‐carrier‐added [ 18 F]FIB on a GE TRACERlab™ FX automated synthesis unit starting from commercially available (4‐iodophenyl)diphenylsulfonium triflate as the labelling precursor. [ 18 F]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 [ 18 F]FIB could be obtained starting from 10.4 GBq of [ 18 F]fluoride. Copyright © 2013 John Wiley & Sons, Ltd.