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Direct incorporation of [18F] into Aliphatic Systems: A promising Mn-catalysed Labelling Technique for PET Imaging

[ Vol. 14 , Issue. 2 ]

Author(s):

Sara Cesarec, Jonathan A. Robson, Laurence S. Carroll*, Eric O. Aboagye and Alan C. Spivey   Pages 101 - 106 ( 6 )

Abstract:


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.

Keywords:

PET, [18F]-Fluoride, aliphatic labelling, imaging, mn-Catalysed, porphyrin, tracer synthesis, nucleophilic fluorination.

Affiliation:

Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Imperial College London, Hammersmith Campus, Du Cane Road, London W12 0NN, Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Imperial College London, Hammersmith Campus, Du Cane Road, London W12 0NN, Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Imperial College London, Hammersmith Campus, Du Cane Road, London W12 0NN, Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Imperial College London, Hammersmith Campus, Du Cane Road, London W12 0NN, Department of Chemistry, Molecular Sciences Research Hub (MSRH), White City Campus, 80 Wood Lane, London W12 0BZ



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