N-Acylation Reactions of Amines

The amide bond is ubiquitous throughout chemistry and is found throughout biology, medicinal chemistry, and materials science. As a consequence, methods for the N-acylation of amines to form amides is one of the most widely researched reactions in organic chemistry. This update describes the most widely used N-acylation reactions used for the preparation of secondary and tertiary amides using a variety of acylating agents, including peptide bond-forming reactions used for the synthesis of large polypeptide chains. The latest developments in N-acylation reactions are also highlighted, in particular, advances in catalytic approaches to amide bonds, chemical ligation of peptides, as well as effective N-acylation strategies that have been employed for the kinetic resolution of racemic amines.