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

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posted on 2016-05-06, 21:07 authored by 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
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.

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