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Oxidation of aromatic lithium thiolates into sulfinate salts: an attractive entry to aryl sulfones labeled with carbon-11
Authors:Martin Claudie  Sandrinelli Franck  Perrio Cécile  Perrio Stéphane  Lasne Marie-Claire
Institution:Laboratoire de Chimie Moléculaire et Thio-Organique (UMR CNRS 6507), ENSICAEN, Université de Caen-Basse Normandie, 6 Boulevard du Maréchal Juin, F-14050 Caen, France.
Abstract:reaction: see text] Aromatic 11C-sulfones were synthesized by S alkylation of lithium arenesulfinates, which are readily available from the corresponding thiols by an oxaziridine-mediated oxidation reaction with 11C]alkyl iodides in THF/H2O (4:1) at 150 degrees C. The radiosyntheses, including purification by HPLC, were completed in an average of 35 min from the end of the bombardment with 55-76% overall radiochemical yields (decay corrected). The described procedure extends the range of accessible labeling methods.
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