期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 19, 页码 4268-4271出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.06.080
关键词
arylsulfones; cyclooxygenase-2; positron emission tomography; Pummerer rearrangement
A general one-pot method has been developed for the conversion of an aryl thiol moiety masked as the butyrate ester to the corresponding C-11-labeled methylsulfone group. The potential of this methodology has been demonstrated by the successful radiosynthesis of carbon-11 analogues of several highly selective cyclooxygenase-2 (COX-2) inhibitors such as Rofecoxib, Etoricoxib and 3-(4-methylsulfonylphenyl)-4-phenyl-5-trifluoromethyl isoxazole in high yield. The chemical and radiochemical purities obtained for the C-11-labeled COX-2 inhibitors are > 99% with a specific activity > 1000 Ci/mmol. (c) 2005 Elsevier Ltd. All rights reserved.
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