Pd-Catalyzed N-arylation of 2-imidazolines Provides Convenient Access to Selective Cyclooxygenase-2 Inhibitors

Title:Pd-Catalyzed N-arylation of 2-imidazolines Provides Convenient Access to Selective Cyclooxygenase-2 Inhibitors

Volume: 10 Issue: 4

Author(s): Mikhail Krasavin

Affiliation:

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

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.

Cite this article as:

Krasavin Mikhail, Pd-Catalyzed N-arylation of 2-imidazolines Provides Convenient Access to Selective Cyclooxygenase-2 Inhibitors, Letters in Organic Chemistry 2013; 10 (4) . https://dx.doi.org/10.2174/1570178611310040002