Two Novel and Efficient Approaches to Synthesis of Enantiopure Dipeptide β-Turn Mimetics: Indolizidinone Amino Acids

Abstract

Indolizidinone amino acids 1 (Figure 1) have been proposed to mimic or induce β-turn secondary structural features for peptides and proteins [1, 2]. It has been demonstrated that incorporation of some of these scaffolds into biologically active peptides has led to peptide mimetic ligands with enhanced activities and metabolic stabilities [1, 2]. However, the lack of efficient methods for the asymmetric synthesis of these compounds is one of the major bottlenecks in the field. Recently we have developed two novel approaches for the synthesis of such compounds in high stereoselectivity.