Abstract

The re-emergence, in the recent years, of cyclooxygenase as a biological target in therapeutic areas other than inflammation is likely to require new optimized leads, particularly suited for the requirements of specific drug development programs. We developed a convenient synthesis of the known imidazole-based selective COX-2 inhibitors bearing primary sulphonamide and methyl sulfone substituents, via Pd-catalyzed imidazoline N-arylation as a key step, followed by dehydrogenation.

Keywords: Buchwald-Hartwig arylation, 2-imidazolines, dehydrogenation, sulphonamide, methyl sulfone, protecting groups, cyclooxygenase inhibitors.