Synthesis of a naphthyridone p38 MAP kinase inhibitor
…, RJ Cvetovich, M McLaughlin, J Amato…
Index: Chung, John Y. L.; Cvetovich, Raymond J.; McLaughlin, Mark; Amato, Joseph; Tsay, Fuh-Rong; Jensen, Mark; Weissman, Steve; Zewge, Daniel Journal of Organic Chemistry, 2006 , vol. 71, # 22 p. 8602 - 8609
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Citation Number: 19
Abstract
Compound 1 is a p38 MAP kinase inhibitor potentially useful for the treatment of rheumatoid arthritis and psoriasis. A novel six-step synthesis suitable for large-scale preparation was developed in support of a drug development program at Merck Research Laboratories. The key steps include a tandem Heck-lactamization, N-oxidation, and a highly chemoselective Grignard addition of 4-(N-tert-butylpiperidinyl) magnesium chloride to a naphthyridone N- ...
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