Pd-Catalyzed N-arylation of 2-imidazolines Provides Convenient Access to Selective Cyclooxygenase-2 Inhibitors
Author(s)
Krasavin, Mikhail
Griffith University Author(s)
Year published
2013
Metadata
Show full item recordAbstract
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.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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Journal Title
Letters in Organic Chemistry
Volume
10
Issue
4
Subject
Organic Chemistry not elsewhere classified
Organic Chemistry