Asymmetric Stepwise Reductive Amination of Aryl N‐Heteroaryl Ketones with Benzyl Amines via Iridium Catalysis

An asymmetric reductive amination of aryl N‐heteroaryl ketones with Benzyl Amines has been realized via one‐pot two‐step process, using p‐toluenesulfonic acid and chiral iridium complexes as catalysts, a mixture of formic acid/triethylamine as a reductant. Twenty‐three examples of chiral aryl N‐heteroaryl methylamines were obtained with good yields and up to 99% ee. Various chiral aryl N‐heteroaryl methylamineswere prepared with good yields and up to 99% enantioselectivity via one‐pot stepwise ketimine formation/asymmetric transfer hydrogenation of aryl N‐heteroaryl ketones and benzyl amines.