Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane

被引：33

作者：

Bauman, A ^{[1
]}

Piel, M ^{[1
]}

Schirrmacher, R ^{[1
]}

Rösch, F ^{[1
]}

机构：

[1] Univ Mainz, Inst Nucl Chem, D-55128 Mainz, Germany

来源：

TETRAHEDRON LETTERS | 2003年 / 44卷 / 51期

关键词：

positron emission tomography; F-18-fluoroethylation; 2-[F-18]fluoroethyl tosylate; 1-bromo-2-[F-18]fluoroethane;

D O I：

10.1016/j.tetlet.2003.10.034

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Radiochemical F-18-fluorination yields of several compounds using the secondary labelling precursors 2-[F-18]fluoroethyl tosylate ([(18)]FETos) and 1-bromo-2-[F-18]fluoroethane ([F-18]BFE) could be considerably enhanced by the addition of an alkali iodide. The radiochemical yield of [F-18]fluoroethyl choline for example could be doubled with [F-18]BFE and increased from 13% to approximate to80% with [F-18]FETos. By addition of alkali iodide to the precursor, the F-18-fluoroethylation yields of established radiopharmaceuticals, especially in the case of automated syntheses, could be significantly increased without major changes of the reaction conditions. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：9165 / 9167

页数：3

共 50 条

[1] Fully Automated Radiosynthesis of 1-(2-[18F]Fluoroethyl)-LTryptophan ([18F]FETrp)
Jiang, Huailei
Guo, Yan
Cai, Hancheng
Viola, Nerissa
Shields, Anthony
Muzik, Otto
Juhasz, Csaba
[J]. NUCLEAR MEDICINE AND BIOLOGY, 2023, 126 : S63 - S63
[2] Copper-mediated reduction of 2-[18F]fluoroethyl azide to 2-[18F]fluoroethylamine
Glaser, Matthias
Arstad, Erik
Gaeta, Alessandra
Nairne, James
Trigg, William
Robins, Edward G.
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2012, 55 (09): : 326 - 331
[3] Radiosynthesis of [18F]fluoromethyl tosylate for [18F]fluoromethylation
Friederike, Beyerlein
Markus, Piel
Tobias, Ross L.
Frank, Roech
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2011, 54 : S483 - S483
[4] 2-[18F]Fluoroethyl tosylate - a versatile tool for building 18F-based radiotracers for positron emission tomography
Kniess, Torsten
Laube, Markus
Brust, Peter
Steinbach, Joerg
[J]. MEDCHEMCOMM, 2015, 6 (10) : 1714 - 1754
[5] Efficient Radiosynthesis of 2-[18F]Fluoroadenosine: A New Route to 2-[18F]Fluoropurine Nucleosides
Marchand, Patrice
Lorilleux, Christophe
Gilbert, Gwenaelle
Gourand, Fabienne
Sobrio, Franck
Peyronnet, Damien
Dhilly, Martine
Barre, Louisa
[J]. ACS MEDICINAL CHEMISTRY LETTERS, 2010, 1 (06): : 240 - 243
[6] A Fully Automated Radiosynthesis of [18F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[18F]Fluoroethyl Tosylate
Schoultz, Bent W.
Reed, Brian J.
Marton, Janos
Willoch, Frode
Henriksen, Gjermund
[J]. MOLECULES, 2013, 18 (06) : 7271 - 7278
[7] Efficient synthesis of 2-bromo-1-[18F]fluoroethane and its application in the automated preparation of 18F-fluoroethylated compounds
Comagic, S
Piel, M
Schirrmacher, R
Höhnemann, S
Rösch, F
[J]. APPLIED RADIATION AND ISOTOPES, 2002, 56 (06) : 847 - 851
[8] Strategy based on kinetics of O-(2-[18F] fluoroethyl)-L-tyrosine ([18F] FET)
Masashi Kameyama
Yumi Umeda-Kameyama
[J]. European Journal of Nuclear Medicine and Molecular Imaging, 2016, 43 : 2267 - 2268
[9] Efficient preparation of 2-[18F] fluorophenylalanine (2-[18F] FPhe) by Cu-mediated radiofluorination
Modemann, D.
Zlatopolskiy, B.
Ermert, J.
Neumaier, B.
[J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2017, 44 : S347 - S347
[10] How to increase the reactivity of [18F]fluoroethyl bromide:: [18F]fluoroethylation of amine, phenol and amide functional groups with [18F]FEtBr, [18F]FEtBr/NaI and [18F]FEtOTf
Zhang, MR
Furutsuka, K
Yoshida, Y
Suzuki, K
[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2003, 46 (06): : 587 - 598

← 1 2 3 4 5 →