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.

Automated summary

An asymmetric reductive amination of aryl N-heteroaryl ketones with Benzyl Amines has been successfully achieved using a one-pot two-step process with p-toluenesulfonic acid and chiral iridium complexes as catalysts and 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.