Enantioselective Synthesis of α‐Substituted Primary Amines by Nucleophilic Addition to Aldehyde‐SAMP Hydrazones

Abstract

The optically active primary amines (R)- or (S)-3 having a center of chirality at the α-position can be obtained from the aldehydes 1 via the SAMP hydrazones (S)-2. Addition of R2Li followed by NN bond cleavage leads in good yields and enantioselectively (ee = 81–94%) to (R)- or (S)-3.