A One-Pot Synthesis of Challenging Chiral Primary Amines

Significance

The conventional synthetic methods for the synthesis of primary amines require multiple steps and harsh nitrogen deprotection conditions, which lead to low overall yield. The authors described a one-pot synthesis of chiral primary amines through an asymmetric reductive amination-hydrogenolysis sequence. In spite of their low reactivity, they achieved the synthesis of ortho-substituted phenylethyl amines in good yield and with high enantioselectivity.