Highly Enantioselective Three-Component Povarov Reaction for Direct Construction of Azaspirocycles,Organic Letters

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Highly Enantioselective Three-Component Povarov Reaction for Direct Construction of Azaspirocycles
Organic Letters ( IF 4.9 ) Pub Date : 2022-08-26 , DOI: 10.1021/acs.orglett.2c02421
Nan-Fang Mo ₁ , Ying Zhang ₁ , Zheng-Hui Guan ₁

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An asymmetric organocatalyzed three-component Povarov reaction to construct azaspirocycles has been developed. A chiral phosphoric acid OCF-CPA bearing o-CF₃-aryl on the H₈–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.

中文翻译：

用于直接构建氮杂螺环的高对映选择性三组分 Povarov 反应

已经开发了一种用于构建氮杂螺环的不对称有机催化三组分波瓦罗夫反应。在 H ₈ -BINOL 框架上带有o -CF ₃ -芳基的手性磷酸OCF-CPA在反应中非常有效。该反应是在以高产率和高对映选择性合成一系列氮杂螺环的理想条件下进行的，从而扩大了传统波瓦罗夫反应的底物范围。

更新日期：2022-08-26

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