A simplified protocol for the automated production of succinimidyl 4-[18F] fluorobenzoate on an IBA Synthera module

被引：23

作者：

Ackermann, Uwe ^{[1
,2
]}

Yeoh, Shinn Dee ^{[1
]}

Sachinidis, John I. ^{[1
]}

Poniger, Stan S. ^{[1
]}

Scott, Andrew M. ^{[1
,2
,3
]}

Tochon-Danguy, Henri J. ^{[1
,2
]}

机构：

[1] Austin Hlth, Ctr Nucl Med & PET, Melbourne, Vic, Australia

[2] Univ Melbourne, Sch Med Dent & Hlth Sci, Melbourne, Vic 3010, Australia

[3] Ludwig Inst Canc Res, Melbourne Austin Branch, Melbourne, Vic, Australia

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2011年 / 54卷 / 9-10期

基金：

英国医学研究理事会;

关键词：

SFB; automated synthesis; protein labelling; nucleophilic aromatic substitution; N-SUCCINIMIDYL;

D O I：

10.1002/jlcr.1892

中图分类号：

Q5 [生物化学];

学科分类号：

070307 [化学生物学];

摘要：

The important peptide labelling reagent succinimidyl 4-[F-18]fluorobenzoate ([F-18]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-[F-18]fluorobenzoate. N,N,N',N'-tetramethyl-O-(N-succinimidyl)uronium tetrafluoroborate (TSTU) was then used to form ([F-18]SFB from 4-[F-18]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 [F-18]SFB was 95.8-98.2%. These simplifications might be of significance to users of other automated synthesis modules.

引用

页码：671 / 673

页数：3

共 9 条

[1]

Two-step radiosynthesis of [18F]N-succinimidyl-4-fluorobenzoate ([18F]SFB) [J].