A general method for the synthesis of aryl [11 C] methylsulfones: potential PET probes for imaging cyclooxygenase-2 expression

…, J Prabhakaran, NR Simpson, RL Van Heertum…

文献索引：Majo, Vattoly J.; Prabhakaran, Jaya; Simpson, Norman R.; Van Heertum, Ronald L.; Mann, J. John; Kumar, J. S. Dileep Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 19 p. 4268 - 4271

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被引用次数: 38

摘要

A general one-pot method has been developed for the conversion of an aryl thiol moiety masked as the butyrate ester to the corresponding 11C-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 ...