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.