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.
Letters in Organic Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/1570178611310040002 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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