One-Pot Catalytic Synthesis of α-Tetrasubstituted Amino Acid Derivatives via In Situ Generation of N-Unsubstituted Ketimines

A one-pot catalytic synthesis of alpha-tetrasubstituted amino acid derivatives via in situ generation of N-unsubstituted ketimines is reported. Because of the irreversible formation of N-unsubstituted ketimines, the yields were higher than those generated under the conventional one-pot reaction conditions. This process prevents the need to isolate unstable N-unsubstituted ketimines with alkyl substituents and streamlines the synthesis of highly congested alpha-amino acid derivatives.

Automated summary

A one-pot catalytic synthesis method for alpha-tetrasubstituted amino acid derivatives via in situ generation of N-unsubstituted ketimines is reported. This approach avoids the need for isolating unstable ketimines, resulting in higher yields and streamlining the synthesis process of highly congested alpha-amino acid derivatives.