An Expeditious Synthesis of the MDM2鈥損53 Inhibitor AM-8553

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• 作者：Brian S. Lucas ; Benjamin Fisher ; Lawrence R. McGee ; Steven H. Olson ; Julio C. Medina ; Eugene Cheung
• 刊名：The Journal of the American Chemical Society
• 出版年：2012
• 出版时间：August 1, 2012
• 年：2012
• 卷：134
• 期：30
• 页码：12855-12860
• 全文大小：473K
• 年卷期：v.134,no.30(August 1, 2012)
• ISSN：1520-5126

文摘

The development of the structurally complex MDM2/p53 inhibitor AM-8553 was impeded by the low yield of the initial synthesis. A second generation synthesis is described that features a Noyori dynamic kinetic resolution, a highly diastereoselective allylation, and a novel oxazoline-assisted piperidinone forming reaction to provide AM-8553 in 35.6% yield and 11 steps.