Catalytic Asymmetric Construction of α,α‐Diaryl Aldehydes via Oxo‐Hydroarylation of Terminal Alkynes

Abstract Chiral aldehydes containing a tertiary stereogenic center are versatile building blocks in organic chemistry. In particular, such structural motifs bearing an α,α‐diaryl moiety are very challenging scaffolds and their efficient asymmetric synthesis is not reported. In this work, a phosphoric acid‐catalyzed enantioselective synthesis of α,α‐diaryl aldehydes from simple terminal alkynes is presented. This approach yields a wide range of highly enolizable α,α‐diaryl aldehydes in good yields with excellent enantioselectivities. Facile transformations of the products, as well as an efficient synthesis of bioactive molecules, including an effective anti‐smallpox agent and an FDA‐approved antidepressant drug (+)‐sertraline, are demonstrated.