Synthesis of imidazole based p38 MAP (mitogen-activated protein) kinase inhibitors under buffered conditions

…, WD Diseroad, CR Nevill, JP Wepsiec

Index: Magnus, Nicholas A.; Diseroad, William D.; Nevill Jr., C. Richard; Wepsiec, James P. Organic Process Research and Development, 2006 , vol. 10, # 3 p. 556 - 560

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Citation Number: 7

Abstract

This article describes chemistry that was developed to give access to multigram quantities of imidazole 479754 and several related analogues for Eli Lilly's p38 MAPK program targeting therapies to address inflammation. The molecules of interest have an isopropyl sulfonyl group present on the 2-aminobenzimidazole heterocycyle that was found to be labile when heated in polar solvents and/or exposed to high or low pH. Due to this instability issue, the ...