A Concise Synthesis of a 尾-Lactamase Inhibitor

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• 作者：Ian K. Mangion ; Rebecca T. Ruck ; Nelo Rivera ; Mark A. Huffman ; Michael Shevlin
• 刊名：Organic Letters
• 出版年：2011
• 出版时间：October 21, 2011
• 年：2011
• 卷：13
• 期：20
• 页码：5480-5483
• 全文大小：703K
• 年卷期：v.13,no.20(October 21, 2011)
• ISSN：1523-7052

文摘

MK-7655 (1) is a 尾-lactamase inhibitor in clinical trials as a combination therapy for the treatment of bacterial infection resistant to 尾-lactam antibiotics. Its unusual structural challenges have inspired a rapid synthesis featuring an iridium-catalyzed N鈥揌 insertion and a series of late stage transformations designed around the reactivity of the labile bicyclo[3.2.1]urea at the core of the target.