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Fully automated, high yielding production of N ‐succinimidyl 4‐[ 18 F]fluorobenzoate ([ 18 F]SFB), and its use in microwave‐enhanced radiochemical coupling reactions
Author(s) -
Scott Peter J. H.,
Shao Xia
Publication year - 2010
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.1785
Subject(s) - yield (engineering) , chemistry , fluorine , radiochemistry , chemical synthesis , coupling reaction , microwave , specific activity , nuclear chemistry , organic chemistry , catalysis , in vitro , physics , enzyme , biochemistry , quantum mechanics , thermodynamics
A General Electric Medical Systems (GEMS) Tracerlab FX FN fluorine‐18 synthesis module has been reconfigured to allow rapid (45 min), fully automated production of N ‐succinimidyl 4‐[ 18 F]fluorobenzoate ([ 18 F]SFB) using the established three‐step, one‐pot synthesis procedure. Purification is by sep‐pak only and [ 18 F]SFB is routinely obtained in 38% non‐decay corrected yield,>1 Ci/µmol specific activity, and >95% radiochemical purity ( n =20). Moreover, this report includes our preliminary research efforts into improving peptide coupling reactions with [ 18 F]SFB using microwave‐enhanced radiochemistry. Reaction times can be reduced by>90%, when compared with traditional thermal reactions, with no significant effect on radiochemical reaction yield. Copyright © 2010 John Wiley & Sons, Ltd.