Development of High-Throughput Experimentation Approaches for Rapid Radiochemical Exploration

Area of Science:

• Radiochemistry
• Chemical Synthesis
• Medical Imaging

Background:

• Positron emission tomography (PET) is crucial for studying physiological processes.
• Current radiolabeling optimization relies on inefficient one-factor-at-a-time methods.
• High-throughput experimentation (HTE) is underutilized in radiochemistry due to short radioisotope lifetimes.

Purpose of the Study:

• To develop and demonstrate an effective HTE workflow for radiochemistry.
• To optimize copper-mediated radiofluorination reactions.
• To explore chemical space for pharmaceutically relevant aryl boronates.

Main Methods:

• Implementation of a novel HTE workflow using commercial equipment.
• Rapid analysis of parallel reactions for optimization.
• Application to copper-mediated radiofluorination of boronate esters.

Main Results:

• Successful adaptation of HTE for radiochemistry challenges.
• Optimization of radiofluorination reactions for pharmaceutical applications.
• Generation of large radiochemistry datasets for further research.

Conclusions:

• The developed HTE workflow overcomes challenges associated with short radioisotope lifetimes.
• This approach accelerates the optimization of PET imaging agents.
• Facilitates exploration of chemical space in radiochemistry for drug discovery.