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

Author(s): Sara Cesarec, Jonathan A. Robson, Laurence S. Carroll*, Eric O. Aboagye, Alan C. Spivey

Journal Name: Current Radiopharmaceuticals

Volume 14 , Issue 2 , 2021

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Graphical 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.

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Article Details

Year: 2021
Published on: 07 September, 2020
Page: [101 - 106]
Pages: 6
DOI: 10.2174/1874471013666200907115026
Price: $65

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