Key Laboratory of Synthetic and Nature Functional Molecule of the Ministry of Education, Department of Chemistry & Materials Science, Northwest University, Xi'an 710127, P.R. China.
Org Lett. 2022 Sep 9;24(35):6397-6401. doi: 10.1021/acs.orglett.2c02421. Epub 2022 Aug 26.
An asymmetric organocatalyzed three-component Povarov reaction to construct azaspirocycles has been developed. A chiral phosphoric acid bearing -CF-aryl on the H-BINOL-framework is highly efficient in the reaction. The reaction was carried out under mind conditions for synthesis of a range of azaspirocycles in high yields and high to excellent enantioselectivities, thus expending the substrate scope of the traditional Povarov reaction.
发展了一种不对称有机催化的三组分 Povarov 反应来构建氮杂螺环化合物。手性磷酸在 H-BINOL 骨架上带有 -CF-芳基,在反应中非常高效。该反应在温和条件下进行,用于合成一系列氮杂螺环化合物,产率高,对映选择性高至优秀,从而扩展了传统 Povarov 反应的底物范围。