ABSTRACT Cyclic β-amino acids have been the subject of a vast amount of research across the chemical, biological, and medicinal disciplines. These molecules are synthetic precursors for a wide variety of useful compounds that include natural products and modified peptides. Many methods have been developed to prepare cyclic β-amino acids. This review will discuss some major approaches for synthesis of cyclic β-amino acid derivatives. These include reductive amination, Curtius rearrangement, Michael addition and cycloaddition approaches. Some interesting cyclic β-amino acid synthetic methods which do not belong to any of the above major approaches will be discussed under miscellaneous strategies.
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