title: Pyrazolo[1,5-a]pyridines as p38 kinase inhibitors.
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.
authors.affiliation: GlaxoSmithKline, Research and Development, Department of Medicinal Chemistry, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. Kirk.L.Stevens@gsk.com
authors.forename: Kirk L
authors.initials: KL
authors.lastname: Stevens
authors.forename: David K
authors.initials: DK
authors.lastname: Jung
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Alberti
authors.forename: Jennifer G
authors.initials: JG
authors.lastname: Badiang
authors.forename: Gregory E
authors.initials: GE
authors.lastname: Peckham
authors.forename: Jim M
authors.initials: JM
authors.lastname: Veal
authors.forename: Mui
authors.initials: M
authors.lastname: Cheung
authors.forename: Philip A
authors.initials: PA
authors.lastname: Harris
authors.forename: Stanley D
authors.initials: SD
authors.lastname: Chamberlain
authors.forename: Michael R
authors.initials: MR
authors.lastname: Peel
mesh_terms: 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*
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011725:Pyridines; D048051:p38 Mitogen-Activated Protein Kinases