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Paper | Regular issue | Vol 78, No. 11, 2009, pp.2811-2826
Published online, 7th September, 2009
DOI: 10.3987/COM-09-11808
Synthesis of Heteroaryl-fused Pyrazoles as P38 Kinase Inhibitors

Sarah C. Abbot, Roland J. Billedeau, Nolan J. Dewdney, Tobias Gabriel, David M. Goldstein, Kristen L. McCaleb,* Michael Soth, Teresa Alejandra Trejo-Martin, and Hasim Zecic

*Department of Medicinal Chemistry, Roche Paolo Alto LLC, 3401 Hillview Avenue, Palo Alto, CA 94304, U.S.A.

Abstract

The synthesis of pyrazolo-pyridine, pyrimidine, pyrazine and pyridazine heterocycles is described. In addition, we report the utilization of 2,4-difluorophenoxide as a leaving group, to facilitate formation of the desired pyrazole adducts.