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

6-l-[F]Fluoro--tyrosine (6-l-[F]FMT) represents a valuable alternative to 6-l-[F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson's disease. However, clinical applications of 6-l-[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-[F]FMT using alcohol-enhanced Cu-mediated radiofluorination of Bpin-substituted chiral Ni(II) complex in the presence of non-basic BuONTf using a volatile PrOH/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-labeling. This method enables an uncomplicated switch between C- and 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-[F]FMT in the clinic.