Single-step radiofluorination of peptides using continuous flow microreactor

Area of Science:

• Radiochemistry
• Medicinal Chemistry
• Chemical Engineering

Background:

• Peptide radiolabelling is crucial for developing diagnostic and therapeutic agents.
• Current radiolabelling methods can be time-consuming and require significant optimization.
• Microfluidic devices offer potential for rapid and efficient chemical synthesis.

Purpose of the Study:

• To develop and optimize a novel microfluidic method for 18F radiolabelling of peptides.
• To investigate the influence of various reaction parameters on radiochemical yield.
• To demonstrate the feasibility of rapid optimization using continuous flow technology.

Main Methods:

• Utilized a continuous flow microfluidic device for 18F radiolabelling of peptides.
• Systematically varied precursor concentration, reaction temperature, and flow rate.
• Evaluated the impact of different leaving groups on the radiolabelling efficiency.

Main Results:

• Achieved successful 18F radiolabelling of peptides in a microfluidic system.
• Identified key parameters influencing radiochemical yields, including precursor concentration, temperature, and flow rate.
• Demonstrated that the choice of leaving group significantly impacts the reaction outcome.

Conclusions:

• Continuous flow microfluidics enables efficient and rapid 18F peptide radiolabelling.
• Reaction optimization is feasible and can be accelerated using this technology.
• This method holds promise for the streamlined development of radiolabelled peptides for medical applications.