American Chemical Society
ol2c02421_si_001.pdf (15.85 MB)

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

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journal contribution
posted on 2022-08-26, 15:05 authored by Nan-Fang Mo, Ying Zhang, Zheng-Hui Guan
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.