Multicomponent Combinatorial Development of Prolyl Pseudo- Peptide Catalysts: Application in the Direct Asymmetric Michael Addition

Oligopeptidic scaffolds are an important class of organocatalysts, which have found remarkable applications in a wide range of catalytic asymmetric transformations. In this way, MCRs may offer a greater promise in the field of peptide catalysis. The classic Ugi-4CR has been successful applied for the preparation of pseudo-peptidic skeletons, including N-alkylated peptides and a wide variety of peptidomimetic by combinatorial procedures – whereas, each of the four starting materials can be easily altered (Scheme 1). Taking into account that the MCRs have not yet been used for organocatalysts discovery, we focused our attention, ton the implementation of Ugi-4CR as a powerful tool to access new class of prolyl pseudo-peptides and therefore, apply them in asymmetric Michael reaction.