Click Chemistry and Radiochemistry: An Update

Area of Science:

• Radiopharmaceutical Chemistry
• Organic Synthesis
• Chemical Biology

Background:

• Click chemistry offers modular and efficient methods for molecular construction.
• The field has expanded beyond copper-catalyzed azide-alkyne cycloaddition to include bioorthogonal reactions.
• Radiopharmaceutical chemistry benefits significantly from click chemistry's unique attributes.

Purpose of the Study:

• To provide a comprehensive overview of recent advancements in click chemistry for radiopharmaceutical applications.
• To highlight emerging trends and the clinical translation of click chemistry-based radiotracers.
• To explore the integration of click chemistry in radiosynthesis and in vivo pretargeting.

Main Methods:

• Review of emergent click transformations applicable to radiosynthesis.
• Analysis of clinical translation of novel radiopharmaceutical probes developed via click chemistry.
• Discussion of click-based in vivo pretargeting strategies for improved imaging.

Main Results:

• Click chemistry has broadened the scope of radiopharmaceutical development.
• Novel click reactions are being integrated into radiosynthesis workflows.
• Successful clinical translation of click chemistry-derived radioprobes is increasing.

Conclusions:

• Click chemistry continues to be a transformative technology in radiopharmaceutical science.
• Emerging click reactions and pretargeting strategies hold significant promise for future diagnostics and therapeutics.
• The field is poised for continued innovation, impacting molecular imaging and targeted radiotherapeutics.