Pyrazolo[1,5-a]pyridines as p38 kinase inhibitors.
[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.
Stevens
Kirk L
KL
GlaxoSmithKline, Research and Development, Department of Medicinal Chemistry, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. Kirk.L.Stevens@gsk.com
Jung
David K
DK
Alberti
Michael J
MJ
Badiang
Jennifer G
JG
Peckham
Gregory E
GE
Veal
Jim M
JM
Cheung
Mui
M
Harris
Philip A
PA
Chamberlain
Stanley D
SD
Peel
Michael R
MR
D018360:Crystallography, X-Ray; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011725:Pyridines; D048051:p38 Mitogen-Activated Protein Kinases