Asymmetric Synthesis of Letermovir Using a Novel Phase-Transfer-Catalyzed Aza-Michael Reaction

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• 作者：Guy R. Humphrey ; Stephen M. Dalby ; Teresa Andreani ; Bangping Xiang ; Michael R. Luzung ; Zhiguo Jake Song ; Michael Shevlin ; Melodie Christensen ; Kevin M. Belyk ; David M. Tschaen
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：June 17, 2016
• 年：2016
• 卷：20
• 期：6
• 页码：1097-1103
• 全文大小：431K
• 年卷期：0
• ISSN：1520-586X

文摘

The development of a concise asymmetric synthesis of the antiviral development candidate letermovir is reported, proceeding in >60% yield over a total of seven steps from commercially available materials. Key to the effectiveness of this process is a novel cinchonidine-based PTC-catalyzed aza-Michael reaction to configure the single stereocenter.