The copper-catalyzed enantioselective C–H arylation between 2-arylindoles and hypervalent iodine reagents has been successfully developed, which provides a convenient and economical route to the highly atroposelective synthesis of axially chiral indole derivatives with a 2-aryl structure (up to 99% ee). Density functional theory calculations and wave function analysis show that the key “sandwich” intermediate leads to high enantioselectivity of the reaction.

Iridium-catalyzed intramolecular asymmetric allylic etherification of salicylic acid derivatives was successfully realized for the first time. By using chiral-bridged biphenyl phosphoramidite ligand L7, a class of novel chiral 1,4-benzoxazepinones was...

A highly efficient palladium‐catalyzed asymmetric synthesis of N‐substituted 4‐quinolones was developed via C−N coupling reaction. Various chiral quinolones were readily obtained with desirable enantioselectivity (up to 95% ee) and excellent yield (up to 99%), enabled by a simple system of palladium acetate and chiral ferrocene bisphosphine as auxiliary ligand. The corresponding racemic derivatives can also be synthesized by a transition metal‐free strategy of potassium hydroxide in DMSO. The influence of temperature on the configurational stability of these C−N axially chiral compounds was also investigated. The efficient functionalization at 3‐position further expands the application range of this synthetic technique.