Facile Synthesis and Chiral Separation of ��-Amino Acid Racemates

Abstract Optically pure ��-amino acids are important components of natural products and essential intermediates of polypeptide and ��-lactam.Traditional preparation methods involved multi-step synthesis,expensive raw materials,complicated operating procedures and low yields.In this paper,a novel approach to get ��-amino acid enantiomers was described.With aldehyde,malonic acid,ammonium acetate as raw materials,five ��-amino acid racemates were synthesized by one-pot method.These amino acids were then resolved by ligand exchange chromatorgraphy(LEC) to yield optically pure ��-amino acids.The results showed that one-pot synthesis of ��-amino acids and chiral separation by LEC was a simple and efficient method,by which the amino acid enantiomers can be produced with low cost and high yield.This method can be adopted for the preparation of ��-amino acid enantiomers with different structures used in the high throughput screening of drug candidates during the process of drug development.

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Received 2008-05-15; published 2008-05-15

Cite this article:

CHEN Feng,CHEN Lei.Facile Synthesis and Chiral Separation of ��-Amino Acid Racemates[J] Chemcial Industry and Engineering, 2008,V25(3): 229-232