Stereocontrolled synthesis of an α–monosubstituted α–amino acid derivative from a Ugi reaction product

Abstract

We report herein an unprecedented concept for an enantiospecific synthetic strategy for α–amino acid derivatives starting from Ugi four-component coupling reaction employing chiral amine, via a chiral morpholinone intermediate. This concept was proven by the successful synthesis of (S)–N–Ac–tert–leucine.