Development of a Practical Synthesis of a p38 Kinase Inhibitor via a Safe and Robust Amination
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- 作者：Zhongping Shi ; Susanne Kiau ; Paul Lobben ; John Hynes ; Jr. ; Hong Wu ; Luca Parlanti ; Robert Discordia ; Wendel W. Doubleday ; Katerina Leftheris ; Alaric J. Dyckman ; Stephen T. Wrobleski ; Konstantinos Dambalas ; Srinivas Tummala ; Simon Leung ; Ehrlic Lo
- 刊名：Organic Process Research & Development
- 出版年：2012
- 出版时间：October 19, 2012
- 年：2012
- 卷：16
- 期：10
- 页码：1618-1625
- 全文大小：349K
- 年卷期：v.16,no.10(October 19, 2012)
- ISSN：1520-586X
文摘
The development of a practical synthesis for a p38 kinase inhibitor is described. The key advances include an improved route to the key intermediate, a substituted pyrrole, and a subsequent animation utilizing O-(4-nitrobenzoyl)hydroxylamine, which provides a safe, scalable, and robust amination method. The new protocol was successfully demonstrated to generate 1.6 kg of API in seven steps and 26% overall yield.