Recent Advances in the Synthesis of Amino Acid Derivatives through Multicomponent Reactions

Abstract Amino acids play significant roles in the study of life sciences, pharmaceutical R&D, bioengineering, and so on. Artificial amino acid‐based drugs are important in advancing therapeutic innovation for multiple diseases including chronic pain, diabetes, and Alzheimer's disease. On the other hand, multicomponent reactions (MCRs) are demonstrated to be a powerful strategy for the construction of complicated structures from readily accessible starting reagents in one pot. Thus, applying multicomponent reactions to the preparation of amino acids and their derivatives can be a potent strategy for advancing the research of pharmaceutical chemistry. With the rapid development of various catalytic methods and multicomponent reactions, this review outlines recent construction methods of amino acid derivatives by transition metal‐catalyzed, light‐mediated and other organocatalytic multicomponent reactions.