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：

071010 ; 081704 ;

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)
Glaser, Matthias
Arstad, Erik
Luthra, Sajinder K.
Robins, Edward G.
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2009, 52 (7-8) : 327 - 330
[2] FLUOROACYLATION AGENTS BASED ON SMALL NCA [F-18] FLUOROCARBOXYLIC ACIDS
GUHLKE, S
COENEN, HH
STOCKLIN, G
[J]. APPLIED RADIATION AND ISOTOPES, 1994, 45 (06) : 715 - 727
[3] ONE-STEP SYNTHESIS OF F-18 LABELED [F-18] N-SUCCINIMIDYL 4-(FLUOROMETHYL)BENZOATE FOR PROTEIN LABELING
LANG, LX
ECKELMAN, WC
[J]. APPLIED RADIATION AND ISOTOPES, 1994, 45 (12) : 1155 - 1163
[4] Labeling G-rich oligonucleotides (GROs) with N-succinimidyl 4-[18F]fluorobenzoate (S18FB)
Li, Junling
Trent, John O.
Bates, Paula J.
Ng, Chin K.
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2006, 49 (14) : 1213 - 1221
[5] Module-assisted synthesis of the bifunctional labelling agent N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB)
Mäding, P
Füchtner, F
Wüst, F
[J]. APPLIED RADIATION AND ISOTOPES, 2005, 63 (03) : 329 - 332
[6] Fully automated preparation of n.c.a. 4-[18F]fluorobenzoic acid and N-succinimidyl 4-[18F]fluorobenzoate using a Siemens/CTI chemistry process control unit (CPCU)
Marik, Jan
Sutcliffe, Julie L.
[J]. APPLIED RADIATION AND ISOTOPES, 2007, 65 (02) : 199 - 203
[7] Fully automated, high yielding production of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB), and its use in microwave-enhanced radiochemical coupling reactions
Scott, Peter J. H.
Shao, Xia
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2010, 53 (09) : 586 - 591
[8] Facile synthesis of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) for protein labeling
Tang, G.
Zeng, Wenbin
Yu, Meixiang
Kabalka, G.
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2008, 51 (1-2) : 68 - 71
[9] Yeoh S, 2009, J LABELLED COMPD RAD, V52, pS289

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