Reactivity of electrochemically concentrated anhydrous [18F]fluoride for microfluidic radiosynthesis of 18F-labeled compounds

被引：31
作者：
Wong, Rebecca [2 ]
Iwata, Ren [1 ,2 ]
Saiki, Hidekazu [3 ]
Furumoto, Shozo [1 ,4 ]
Ishikawa, Yoichi [1 ]
Ozeki, Eiichi [3 ]
机构：
[1] Tohoku Univ, Ctr Cyclotron & Radioisotope, Sendai, Miyagi 9808578, Japan
[2] Tohoku Univ, Grad Sch Pharmaceut Sci, Sendai, Miyagi 9808578, Japan
[3] Shimadzu Co Ltd, Technol Res Lab, Kyoto 6190237, Japan
[4] Tohoku Univ, Grad Sch Med, Sendai, Miyagi 9808575, Japan
来源：
APPLIED RADIATION AND ISOTOPES | 2012年 / 70卷 / 01期
基金：
日本科学技术振兴机构; 日本学术振兴会;
关键词：
Microfluidics; Radiosynthesis; F-18; F-18]fluoride; PET probe; POSITRON-EMISSION-TOMOGRAPHY; PET; FLUOROMISONIDAZOLE;
D O I：
10.1016/j.apradiso.2011.09.022
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
In order to demonstrate the usefulness of electrochemically concentrated [F-18]fluoride the reactivity of the [K+/K.222] F-18(-) complex concentrated in an aprotic solvent (ca. 60 mu L) was evaluated via nucleophilic F-18-substitution reactions through radiosynthesis of [F-18]FDG, [F-18]FMISO, [F-18]flumazenil and [F-18]fluoromethyl bromide. The substitutions were carried out in a microfluidic reaction flow cell and the effects of reaction time, temperature, precursor concentration and reaction solvent on the F-18-substitution yields were investigated. The F-18-fluorination yields for the four F-18-labeled compounds under optimized conditions (98% for protected [F-18]FDG, 80% for protected [F-18]FMISO, 20% for [F-18]flumazenil and 60% for [F-18]fluoromethyl bromide) were comparable to or higher than those obtained by conventional means. In this study it is clearly demonstrated that electrochemically concentrated [F-18]fluoride enables microfluidic radiosynthesis by effectively reducing synthesis times and especially by increasing radiochemical yields of products labile at high temperatures. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：193 / 199
页数：7
相关论文
共 21 条
[1]   Positron emission tomography (PET) and microfluidic devices: A breakthrough on the microscale? [J].
Audrain, Helen .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2007, 46 (11) :1772-1775
[2]   Synthesis of hypoxia imaging agent 1-(5-deoxy-5-fluoro-α-D-arabinofuranosyl)-2-nitroimidazole using microfluidic technology [J].
Bouvet, Vincent R. ;
Wuest, Melinda ;
Wiebe, Leonard I. ;
Wuest, Frank .
NUCLEAR MEDICINE AND BIOLOGY, 2011, 38 (02) :235-245
[3]  
BRADY F, 2003, Patent No. 03078358
[4]   Chemistry with [18F]fluoride ion [J].
Cai, Lisheng ;
Lu, Shuiyu ;
Pike, Victor W. .
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2008, 2008 (17) :2853-2873
[5]   Microfluidic reactor for the radiosynthesis of PET radiotracers [J].
Gillies, JM ;
Prenant, C ;
Chimon, GN ;
Smethurst, GJ ;
Perrie, W ;
Hambletta, I ;
Dekker, B ;
Zweit, J .
APPLIED RADIATION AND ISOTOPES, 2006, 64 (03) :325-332
[6]   No-carrier-added nucleophilic 18F-labelling in an electrochemical cell exemplified by the routine production of [18F]altanserin [J].
Hamacher, K. ;
Coenen, H. H. .
APPLIED RADIATION AND ISOTOPES, 2006, 64 (09) :989-994
[7]  
HAMACHER K, 1986, J NUCL MED, V27, P235
[8]   [18F]Fluoromethyl triflate, a novel and reactive [18F]fluoromethylating agent:: preparation and application to the on-column preparation of [18F]fluorocholine [J].
Iwata, R ;
Pascali, C ;
Bogni, A ;
Furumoto, S ;
Terasaki, K ;
Yanai, K .
APPLIED RADIATION AND ISOTOPES, 2002, 57 (03) :347-352
[9]   Preparation of fluorine-18-labelled fluoromisonidazole using two different synthesis methods [J].
Kämäräinen, EL ;
Kyllönen, T ;
Nihtilä, O ;
Björk, H ;
Solin, O .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2004, 47 (01) :37-45
[10]   Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics [J].
Lee, CC ;
Sui, GD ;
Elizarov, A ;
Shu, CYJ ;
Shin, YS ;
Dooley, AN ;
Huang, J ;
Daridon, A ;
Wyatt, P ;
Stout, D ;
Kolb, HC ;
Witte, ON ;
Satyamurthy, N ;
Heath, JR ;
Phelps, ME ;
Quake, SR ;
Tseng, HR .
SCIENCE, 2005, 310 (5755) :1793-1796
123