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A simplified protocol for the automated production of succinimidyl 4‐[ 18 F]fluorobenzoate on an IBA Synthera module
Author(s) -
Ackermann Uwe,
Yeoh Shinn Dee,
Sachinidis John I.,
Poniger Stan S.,
Scott Andrew M.,
TochonDanguy Henri J.
Publication year - 2011
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.1892
Subject(s) - chemistry , tetramethylammonium hydroxide , reagent , hydrolysis , trifluoromethanesulfonate , labelling , yield (engineering) , tetrafluoroborate , acetic acid , hydroxide , aqueous solution , ammonium hydroxide , tetramethylammonium , radiochemistry , nuclear chemistry , organic chemistry , catalysis , ionic liquid , ion , biochemistry , materials science , metallurgy
The important peptide labelling reagent succinimidyl 4‐[ 18 F]fluorobenzoate ([ 18 F]SFB) has been synthesised in 75–85% decay corrected radiochemical yield using the IBA Synthera platform (IBA Cyclotron Solutions, Louvain‐la‐neuve, Belgium) with the fluorodeoxyglucose‐integrated fluidic processor nucleophilic and only four reagent vials in a single reactor. (4‐ethoxycarbonylphenyl) trimethylammonium triflate was used as the labelling precursor and 1 M aqueous tetramethylammonium hydroxide for the hydrolysis of the intermediate ethyl 4‐[ 18 F]fluorobenzoate. N,N,N′,N′‐tetramethyl‐O‐(N‐succinimidyl)uronium tetrafluoroborate (TSTU) was then used to form [ 18 F]SFB from 4‐[ 18 F]fluorobenzoate. By omitting the addition of acetic acid and introducing a combined hydrolysis/water removal step, the synthesis time was shortened to 58 minutes. After SepPak purification, the radiochemical purity of [ 18 F]SFB was 95.8–98.2%. These simplifications might be of significance to users of other automated synthesis modules.