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

被引：43

作者：

Humphrey, Guy R. ^{[1
]}

Dalby, Stephen M. ^{[1
]}

Andreani, Teresa ^{[1
]}

Xiang, Bangping ^{[1
]}

Luzung, Michael R. ^{[1
,2
]}

Song, Zhiguo Jake ^{[1
]}

Shevlin, Michael ^{[1
]}

Christensen, Melodie ^{[1
]}

Belyk, Kevin M. ^{[1
]}

Tschaen, David M. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Proc Chem, POB 2000, Rahway, NJ 07065 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Proc Res & Dev, 1 Squibb Dr, New Brunswick, NJ 08903 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2016年 / 20卷 / 06期

关键词：

ANTICYTOMEGALOVIRUS COMPOUND AIC246; HUMAN-CYTOMEGALOVIRUS; RESISTANCE;

D O I：

10.1021/acs.oprd.6b00076

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

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.

引用

页码：1097 / 1103

页数：7

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