917389-34-5Relevant articles and documents
Asymmetric synthesis of letermovir using a novel phase-Transfer-catalyzed aza-michael reaction
Humphrey, Guy R.,Dalby, Stephen M.,Andreani, Teresa,Xiang, Bangping,Luzung, Michael R.,Song, Zhiguo Jake,Shevlin, Michael,Christensen, Melodie,Belyk, Kevin M.,Tschaen, David M.
, p. 1097 - 1103 (2016)
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 nove
Combining traditional 2D and modern physical organic-derived descriptors to predict enhanced enantioselectivity for the key aza-Michael conjugate addition in the synthesis of Prevymis (letermovir)
Mets?nen, Toni T.,Lexa, Katrina W.,Santiago, Celine B.,Chung, Cheol K.,Xu, Yingju,Liu, Zhijian,Humphrey, Guy R.,Ruck, Rebecca T.,Sherer, Edward C.,Sigman, Matthew S.
, p. 6922 - 6927 (2018/09/11)
Quantitative structure-activity relationships have an extensive history for optimizing drug candidates, yet they have only recently been applied in reaction development. In this report, the predictive power of multivariate parameterization has been explored toward the optimization of a catalyst promoting an aza-Michael conjugate addition for the asymmetric synthesis of letermovir. A hybrid approach combining 2D QSAR and modern 3D physical organic parameters performed better than either approach in isolation. Using these predictive models, a series of new catalysts were identified, which catalyzed the reaction to provide the desired product in improved enantioselectivity relative to the parent catalyst.
METHOD FOR PRODUCING DIHYDROQUINAZOLINES
-
Page/Page column 35-36, (2008/06/13)
The present invention relates to a method for producing dihydroquinazolines of formula (I), which are used to manufacture medicaments.