Article (Scientific journals)
Ring-Closing Synthesis of Dibenzothiophene Sulfonium Salts and Their Use as Leaving Groups for Aromatic 18F-Fluorination
Gendron, Thibault; Sander, Kerstin; Cybulska, Klaudia et al.
2018In Journal of the American Chemical Society, 140 (35), p. 11125–11132
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Keywords :
Chemistry; Radiolabeling; Precursors; Aromatic compounds; Cyclization; Nuclear Imaging
Abstract :
[en] 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 [18F]fluoride to give [18F]fluoroarenes in predictable radiochemical yields. The strategy expands the available radiochemical space and provides superior labeling efficiency for clinically relevant PET tracers.
Research Center/Unit :
Institute of Nuclear Medicine, University College London
Department of Chemistry, University College London
Disciplines :
Chemistry
Radiology, nuclear medicine & imaging
Author, co-author :
Gendron, Thibault  ;  Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique-nucléaire
Sander, Kerstin
Cybulska, Klaudia
Benhamou, Laure
Sin, PakKwanBrian
Khan, Aqsa
Wood, Michael
Porter, MichaelJ.
Årstad, Erik
Language :
English
Title :
Ring-Closing Synthesis of Dibenzothiophene Sulfonium Salts and Their Use as Leaving Groups for Aromatic 18F-Fluorination
Publication date :
August 2018
Journal title :
Journal of the American Chemical Society
ISSN :
0002-7863
eISSN :
1520-5126
Publisher :
American Chemical Society (ACS)
Volume :
140
Issue :
35
Pages :
11125–11132
Peer reviewed :
Peer Reviewed verified by ORBi
European Projects :
FP7 - 602102 - EPITARGET - Targets and biomarkers for antiepileptogenesis
Name of the research project :
EPITARGET - Targets and biomarkers for antiepileptogenesis
Funders :
EU - European Union
Leonard Wolfson Experimental Neurology Centre, Mallinckrodt
UCL Business
Wellcome Trust
CRUK - Cancer Research UK
EPSRC - Engineering and Physical Sciences Research Council
Funding number :
602102; C1519/A16463; 102407/Z/13/Z
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