Production of 6-<span style="font-variant: small-caps">l</span>-[¹⁸F]Fluoro-<i>m</i>-tyrosine in an Automated Synthesis Module for ¹¹C-Labeling

Abstract

6-l-[18F]Fluoro-m-tyrosine (6-l-[18F]FMT) represents a valuable alternative to 6-l-[18F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson’s disease. However, clinical applications of 6-l-[18F]FMT have been limited by the paucity of practical production methods for its automated production. Herein we describe the practical preparation of 6-l-[18F]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 11C-labeling. This method enables an uncomplicated switch between 11C- and 18F-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-[18F]FMT in the clinic.

Keywords

• fluorine-18
• radiofluorination
• Cu-mediated
• alcohol-enhanced
• l-[¹⁸F]fluoro-m-tyrosine%22%2C%22default_operator%22%3A%22AND%22%7D%7D%7D"> 6-<span style="font-variant: small-caps">l</span>-[¹⁸F]fluoro-<i>m</i>-tyrosine
• automated synthesis