Background:
One of the challenges in positron emission tomography (PET) is labelling complex aliphatic
molecules.
Objective:
To develop a method of metal-catalysed radiofluorination that is site-selective and works in moderate to good
yields under facile conditions.
Methods:
We report here 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 are reported. Radiochemical
Incorporations (RCIs) up to 69% were achieved within 60 min without the need for pre-activation or specialist equipment.
Conclusion:
The method features mild conditions (60 °C) and promises to constitute a valuable approach to labelling of
biomolecules and drug substances.