Highly Enantioselective Three-Component Povarov Reaction for Direct Construction of Azaspirocycles.
Nan-Fang MoYing ZhangZheng-Hui GuanPublished in: Organic letters (2022)
An asymmetric organocatalyzed three-component Povarov reaction to construct azaspirocycles has been developed. A chiral phosphoric acid OCF-CPA bearing o -CF 3 -aryl on the H 8 -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.