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Synthesis of Axially Chiral Biaryl Compounds

July 29, 2025

Axially chiral biaryl frameworks are important structural units widely found in pharmaceutical molecules and natural products, such as the clinically used antibiotic vancomycin. In addition, these frameworks serve as privileged ligands and catalysts and are extensively applied in asymmetric synthesis. Due to their favorable biological activities and potential applications in asymmetric catalysis, the asymmetric synthesis of axially chiral biaryl compounds has attracted considerable attention from chemists.

Currently, the construction of axially chiral biaryl phosphine compounds mainly relies on transition metal-catalyzed asymmetric coupling and C–H functionalization reactions. Developing efficient catalytic systems and novel synthetic methodologies for the diverse construction of such compounds holds significant research and application value. In our work, we employed bifunctional chiral quaternary phosphonium salts to catalyze an asymmetric tandem arylation reaction between nitroolefins and allylmalononitriles, achieving the stereoselective construction of axially chiral biaryl phosphine compounds and providing a new approach for their synthesis.

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