Recent Advances in Synthetic Methodologies to Form C-¹⁸F Bonds

Area of Science:

• Radiochemistry
• Organic Synthesis
• Molecular Imaging

Background:

• Positron Emission Tomography (PET) is vital for early disease diagnosis.
• Fluorine-18 is a key isotope for PET tracers due to its properties.
• Efficiently synthesizing C-18F bonds is a major focus in organic chemistry and radiochemistry.

Purpose of the Study:

• To review recent advances (2015-2021) in the organic synthesis of C-18F bonds.
• To cover various synthetic strategies for incorporating Fluorine-18 into molecules.
• To highlight the progress in developing PET tracers.

Main Methods:

• Review of non-catalytic radiofluorinations using good leaving groups.
• Analysis of transition metal-catalyzed radiofluorinations.
• Examination of photo- or electro-catalytic synthetic radiofluorinations.

Main Results:

• Significant progress has been made in developing efficient and mild methods for C-18F bond formation.
• Diverse synthetic strategies, including catalytic and non-catalytic approaches, have advanced the field.
• The review covers methods published between 2015 and 2021.

Conclusions:

• Organic synthetic methods for forming C-18F bonds are rapidly evolving.
• Continued advancements are expected to drive the development of novel PET tracers.
• This field is critical for improving early disease diagnosis through molecular imaging.