Direct incorporation of [18F] into Aliphatic Systems: a promising Mn-catalysed labelling technique for PET imaging
File(s)
Accepted version
Author(s)
Cesarec, Sara
Robson, Jonathan A
Carroll, Laurence S
Aboagye, Eric O
Spivey, Alan C
Type
Journal Article
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.
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.
Date Issued
2020-09-07
Date Acceptance
2020-08-05
Citation
Current Radiopharmaceuticals, 2020, 13
ISSN
1874-4710
Publisher
Bentham Science Publishers
Journal / Book Title
Current Radiopharmaceuticals
Volume
13
Copyright Statement
© 2020 Bentham Science Publishers. All rights reserved.
Identifier
https://www.ncbi.nlm.nih.gov/pubmed/32895047
PII: CRP-EPUB-109752
Subjects
PET
[18F]-Fluoride
aliphatic labelling
imaging
mn-Catalysed
porphyrin
tracer synthesis
nucleophilic fluorination
Publication Status
Published
Coverage Spatial
United Arab Emirates
Date Publish Online
2020-09-07