Pyrazolo[1,5-a]pyridines as p38 Kinase Inhibitors
Kirk L. Stevens(GlaxoSmithKline (United States)), David Jung(Research Triangle Park Foundation), Michael J. Alberti(Research Triangle Park Foundation), Jennifer G. Badiang(Research Triangle Park Foundation), Gregory E. Peckham(GlaxoSmithKline (United States)), Jim M. Veal(GlaxoSmithKline (United States)), Mui Cheung(GlaxoSmithKline (United States)), Philip A. Harris(GlaxoSmithKline (United States)), Stanley D. Chamberlain(GlaxoSmithKline (United States)), Michael Peel(GlaxoSmithKline (United States))
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Abstract
[reaction: see text] A convergent synthesis of substituted pyrazolo[1,5-a]pyridines has been achieved either via a regioselective [3 + 2] cycloaddition of N-aminopyridines with alkynes or by thermal cyclization of disubstituted azirines. Subsequent palladium-catalyzed introduction of pyridines or de novo synthesis of pyrimidines affords inhibitors of p38 kinase.
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