Production of 6-l-[18F]Fluoro-m-tyrosine in an Automated Synthesis Module for 11C-Labeling

被引:3
作者
Orlovskaya, Viktoriya V. [1 ]
Craig, Austin S. [2 ,3 ]
Fedorova, Olga S. [1 ]
Kuznetsova, Olga F. [1 ]
Neumaier, Bernd [2 ,3 ,4 ]
Krasikova, Raisa N. [1 ]
Zlatopolskiy, Boris D. [2 ,3 ,4 ]
机构
[1] NP Bechtereva Inst Human Brain, St Petersburg 197376, Russia
[2] Forschungszentrum Julich, Inst Neurosci & Med, INM 5 Nucl Chem, D-52425 Julich, Germany
[3] Univ Clin Cologne, Inst Radiochem & Expt Mol Imaging, D-50937 Cologne, Germany
[4] Max Planck Inst Metab Res, D-50931 Cologne, Germany
来源
MOLECULES | 2021年 / 26卷 / 18期
关键词
fluorine-18; radiofluorination; Cu-mediated; alcohol-enhanced; 6-l-[F-18]fluoro-m-tyrosine; automated synthesis; PARKINSONS-DISEASE; AMINO-ACIDS; CURIE LEVEL; M-TYROSINE; L-DOPA; RADIOFLUORINATION; F-18-FLUORINATION; TRACERS; ANALOGS; ESTERS;
D O I
10.3390/molecules26185550
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
6-l-[F-18]Fluoro-m-tyrosine (6-l-[F-18]FMT) represents a valuable alternative to 6-l-[F-18]FDOPA which is conventionally used for the diagnosis and staging of Parkinson's disease. However, clinical applications of 6-l-[F-18]FMT have been limited by the paucity of practical production methods for its automated production. Herein we describe the practical preparation of 6-l-[F-18]FMT using alcohol-enhanced Cu-mediated radiofluorination of Bpin-substituted chiral Ni(II) complex in the presence of non-basic Bu4ONTf using a volatile iPrOH/MeCN mixture as reaction solvent. A simple and fast radiolabeling procedure afforded the tracer in 20.0 +/- 3.0% activity yield within 70 min. The developed method was directly implemented onto a modified TracerLab FX C Pro platform originally designed for C-11-labeling. This method enables an uncomplicated switch between C-11- and F-18-labeling. The simplicity of the developed procedure enables its easy adaptation to other commercially available remote-controlled synthesis units and paves the way for a widespread application of 6-l-[F-18]FMT in the clinic.
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页数:13
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