Single-step radiofluorination of peptides using continuous flow microreactor

Abstract

18F radiolabelling of peptides bearing two different prosthetic groups was successfully conducted in a continuous flow microfluidic device for the first time. Radiochemical yields were dependent on precursor concentration, reaction temperature and flow rate. The choice of leaving group had a dramatic influence on the reaction outcome. Rapid reaction optimization was possible.

Managing Hazardous Reactions and Compounds in Process Chemistry

“…The incorporation of a fluorine radiolabel into diagnostic agents lends itself to rapid flow reactions (152). The half-life of 18 F is very short, about 20 minutes, thus flow systems that incorporate more than one operation are good means to make these ephemeral molecules.…”

Boron–18F containing positron emission tomography radiotracers: advances and opportunities

“…Recently, a promising method for single-step radiofluorination of peptides using a continuous flow microreactor was described, but further development is still required (14). Recently, a promising method for single-step radiofluorination of peptides using a continuous flow microreactor was described, but further development is still required (14).…”

“…All of these approaches for biomolecule radiofluorination generally require multistep reactions that lead to long reaction times, formation of by-products and the requirement for efficient optimized purification methods. Recently, a promising method for single-step radiofluorination of peptides using a continuous flow microreactor was described, but further development is still required (14). Nevertheless, the application of microreactors in radiofluorinations of small molecules is already a reality that has delivered results, leading us to infer that this will be an important technique in the future of radiochemistry owing to the compatibility with small amounts of materials, fine control of the reaction parameters and improved radiosynthesis efficiency (15).…”

Microfluidics for Synthesis of Peptide-Based PET Tracers

“…Direct radiolabelling of peptides with 18 F-fluoride was also successfully achieved using the Advion NanoTek continuous flow microreactor [ 45 ]. These results showed radiochemical yields were dependent on the leaving group, precursor concentration, reaction temperature, and flow rate.…”