Background: One of the challenges in positron emission tomography (PET) is labelling
complex aliphatic molecules.
Objective: This study aimed to develop a method of metal-catalysed radiofluorination that is site-selective
and works in moderate to good yields under facile conditions.
Methods: Herein, we report on the optimisation of an aliphatic C-H to C-18F bond transformation
catalysed by a Mn(porphyrin) complex.
Results: The successful oxidation of 11 aliphatic molecules, including progesterone, is reported.
Radiochemical Incorporations (RCIs) up to 69% were achieved within 60 min without the need for
pre-activation or special equipment.
Conclusion: The method features mild conditions (60 °C) and promises to constitute a valuable approach
to labelling of biomolecules and drug substances.