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. 2005 Oct 1;15(19):4268-71.
doi: 10.1016/j.bmcl.2005.06.080.

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

Vattoly J Majo  1 , Jaya Prabhakaran, Norman R Simpson, Ronald L Van Heertum, J John Mann, J S Dileep Kumar
Affiliations

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

Vattoly J Majo et al. Bioorg Med Chem Lett. .

Abstract

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 isoxazole in high yield. The chemical and radiochemical purities obtained for the 11C-labeled COX-2 inhibitors are >99% with a specific activity >1000 Ci/mmol.

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