Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 140, Issue 35, Pages 11125-11132Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jacs.8b06730
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Funding
- European Union's Seventh Framework Programme (FP7/2007-2013) [602102]
- Leonard Wolfson Experimental Neurology Centre, Mallinckrodt
- UCL Business [HFSE PoC-13-003]
- Wellcome Trust [102407/Z/13/Z]
- Clinical Research and Development Committee Research Funding from the BRC/UCLH Charities [F196]
- CRUK & EPSRC Comprehensive Cancer Imaging Centre at KCL & UCL - Cancer Research UK [C1519/A16463]
- CRUK & EPSRC Comprehensive Cancer Imaging Centre at KCL & UCL - Engineering and Physical Sciences Research Council (EPSRC) [C1519/A16463]
- EPSRC Case Studentship
- GE
- UCL MSci in Chemistry
- UCL MRes Organic Chemistry: Drug Discovery Programme
- Reta Lila Weston Institute for Neurological Studies
- Progressive Supra nuclear Palsy (Europe) Association
- Department of Health's NIHR Biomedical Research Centres funding scheme
- EPSRC [EP/K005030/1, EP/P020410/1] Funding Source: UKRI
- Wellcome Trust [102407/Z/13/Z] Funding Source: Wellcome Trust
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Herein, we report a novel intramolecular ring-closing reaction of biaryl thioethers that give access to highly functionalized dibenzothiophene sulfonium salts under mild conditions. The resulting precursors react regioselectively with [F-18]fluoride to give [F-18]fluoroarenes in predictable radiochemical yields. The strategy expands the available radiochemical space and provides superior labeling efficiency for clinically relevant PET tracers.
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