Development of a Practical Synthesis of a Pyrazolopyridinone-Based p38 MAP Kinase Inhibitor

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• 作者：Robert R. Milburn ; Oliver R. Thiel ; Michal Achmatowicz ; Xiang Wang ; Jamie Zigterman ; Charles Bernard ; John T. Colyer ; Evan DiVirgilio ; Rich Crockett ; Tiffany L. Correll ; Karthik Nagapudi ; Kumar Ranganathan ; Simon J. Hedley ; Alan Allgeier ; Robert D. Larsen
• 刊名：Organic Process Research & Development
• 出版年：2011
• 出版时间：January 21, 2011
• 年：2011
• 卷：15
• 期：1
• 页码：31-43
• 全文大小：487K
• 年卷期：v.15,no.1(January 21, 2011)
• ISSN：1520-586X

文摘

A practical synthesis of the pyrazolopyridinone-based p38 MAP kinase inhibitor (4) was required for an ongoing program. The synthesis of a key pyrazolopyridinone building block was refined and optimized to provide kilogram quantities of 10 without chromatography or extractive workups. An efficient building-block strategy was employed to give optimal control of the key quality attributes, and in situ Raman spectroscopy was used to monitor and understand the complex solid-state properties of 4.