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Synfacts 2009(7): 0701-0701  
DOI: 10.1055/s-0029-1217243
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a p38 MAP Kinase Inhibitor

Contributor(s): Philip Kocienski
M. Achmatowicz*, O. R. Thiel, P. Wheeler, C. Bernard, J. Huang, R. D. Larsen, M. M. Faul
Amgen Inc., Thousand Oaks, USA
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Publikationsverlauf

Publikationsdatum:
22. Juni 2009 (online)

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Significance

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.