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Recently, researchers from Xiamen University and Zhejiang University have implemented a series of catalytic asymmetric dearomatization reactions based on the direct activation of carbon-carbon triple bonds by chiral phosphoric acid through a hydrogen bond-oriented tight ion pair strategy to establish chirality.
Organic acid directly activates a new type of alkynyl reaction mode
.
The reaction is catalyzed by chiral Bronsted acid based on the direct activation of carbon-carbon triple bonds.
It has excellent chemical selectivity, regioselectivity and enantioselectivity, as well as good substrate universality, and is compatible with naphthol and phenol.
Various aromatic rings such as pyrrole and pyrrole can realize the high-atom economic synthesis of a series of chiral quaternary carbon-centered spirocyclic compounds, providing broad application prospects for organic synthesis and medicinal chemistry
.
The researchers also used density functional theory calculations to clearly analyze the asymmetric induction mode of this type of ring-forming reaction
This research work not only provides a new activation mode for chiral organic acid catalysis, but also provides a new way and new method for the highly enantioselective synthesis of pharmaceutical active molecules
