Enantioselective Synthesis of Axially Chiral Heterobiaryl N‐Cbz‐Protected Diamines via Organocatalytic Arylation of 5‐Aminoisoxazoles.

An enantioselective arylation of isoxazoles with N‐Cbz‐protected azonaphthalenes is disclosed, affording a range of axially chiral arylisoxazoles in good yields and excellent enantiocontrol by utilizing chiral phosphoric acid. Cbz protecting group can be readily removed, resulting in five‐six membered axially chiral heterobiaryl amines bearing free amine maintaining enantiomeric purity. [ABSTRACT FROM AUTHOR]