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Synthesis of a p38 MAP Kinase Inhibitor
M. Achmatowicz*, O. R. Thiel, P. Wheeler, C. Bernard, J. Huang, R. D. Larsen, M. M. Faul
Amgen Inc., Thousand Oaks, USA
22 June 2009 (online)
p38 Mitogen-activated protein (MAP) kinase inhibitors are potential agents for the treatment of inflammatory diseases such as rheumatoid arthritis, Crohn’s disease and psoriasis. A detailed refinement of the discovery route to the target molecule is described which features a one-pot synthesis of the boronic acid I and its Suzuki coupling to the phthalazine derivative E. The order of bond construction was important for success.