926657-23-0Relevant articles and documents
Dynamic kinetic resolution: Asymmetrie transfer hydrogenation of α-alkyl-substituted β-ketoamides
Limanto, John,Krska, Shane W.,Dorner, Benjamin T.,Vazquez, Enrique,Yoshikawa, Naoki,Tan, Lushi
supporting information; experimental part, p. 512 - 515 (2010/05/02)
[Chemical equation presented] Dynamic kinetic resolution (deracemization) of various a-alkyl-substituted β-ketoamides 1 via asymmetric transfer hydrogenation proceeded efficiently to give the corresponding syn-β-hydroxy amides 3 in high diastereo- and enantioselectivities. Specifically, subjection of 1 to HCO2H and Et3N in the presence of 0.5-1 mol % of pentafluorobenzenesulfonyl-DPEN-Ru catalyst 2b at 30-40 °C in either PhCH3 or CH2Cl2 generated the syn-hydroxy product 3 selectively in 15-33:1 dr, 93-97% ee, and 75-88% isolated yields.
Ezetimibe analogs with a reorganized azetidinone ring: Design, synthesis, and evaluation of cholesterol absorption inhibitions
Xu, Xianxiu,Fu, Renzhong,Chen, Jin,Chen, Shengwu,Bai, Xu
, p. 101 - 104 (2007/10/03)
The underlying principle of drug design in this paper is that the maximum retention of the functional groups that exist in the marketed drug would provide a higher probability for comparable safety while the conformational changes in the newly created ana