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

在自动化合成模块中生产 6-l-[(18)F]氟-间-酪氨酸用于 (11)C 标记

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Abstract

6-l-[(18)F]Fluoro-m-tyrosine (6-l-[(18)F]FMT) represents a valuable alternative to 6-l-[(18)F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson's disease. However, clinical applications of 6-l-[(18)F]FMT have been limited by the paucity of practical production methods for its automated production. Herein we describe the practical preparation of 6-l-[(18)F]FMT using alcohol-enhanced Cu-mediated radiofluorination of Bpin-substituted chiral Ni(II) complex in the presence of non-basic Bu(4)ONTf 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 (11)C-labeling. This method enables an uncomplicated switch between (11)C- and (18)F-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-[(18)F]FMT in the clinic.

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