Facile and Rapid Synthesis of alpha-Amidoester Derivatives Based on the Three-Component Passerini Reaction (P-3CR)

Modification of biologically active ethyl-3-bromopyruvate (Et-3-BrP), using the Passerini three-component reaction, to fully substitute -amidoester (-dicarbonyl) derivatives was investigated. The method is efficient for the one-step preparation of highly functionalized -dicarbonyl derivatives containing N-protected amino acid residues and aliphatic, aromatic, and heteroaromatic carboxylic ester derivatives.