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.
Original language | English (US) |
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Pages (from-to) | 101-106 |
Number of pages | 6 |
Journal | Current Radiopharmaceuticals |
Volume | 14 |
Issue number | 2 |
DOIs | |
State | Published - 2021 |
Keywords
- Aliphatic labelling
- Imaging
- Mn-Catalysed
- Nucleophilic fluorination
- PET
- Porphyrin
- Tracer synthesis
- [F]-Fluoride
ASJC Scopus subject areas
- Radiology Nuclear Medicine and imaging
- Pharmacology