Synthesis of a naphthyridone p38 MAP kinase inhibitor

…, RJ Cvetovich, M McLaughlin, J Amato…

文献索引：Amato, Joseph S.; Chung, John Y. L.; Cvetovich, Raymond J.; Gong, Xiaoyi; McLaughlin, Mark; Reamer, Robert A. Journal of Organic Chemistry, 2005 , vol. 70, # 5 p. 1930 - 1933

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被引用次数: 19

摘要

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- ...