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

Author(s): Mikhail Krasavin.

Journal Name: Letters in Organic Chemistry

Volume 10 , Issue 4 , 2013

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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.

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Article Details

Year: 2013
Page: [235 - 239]
Pages: 5
DOI: 10.2174/1570178611310040002
Price: $65

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