The carbamate group is a key structural motif in many approved drugs and prodrugs. There is an increasing use of carbamates in medicinal chemistry and many derivatives are specifically designed to make drug–target interactions through their carbamate moiety. In this Perspective, we present properties and stabilities of carbamates, reagents and chemical methodologies for the synthesis of carbamates, and recent applications of carbamates in drug design and medicinal chemistry.

This review discusses the use of flow chemistry as versatile tool for the synthesis and derivatisation of privileged scaffolds, looking at applicability, diversity-oriented synthesis options, inherent sustainability and green chemistry aspects.

Formation of amide bonds is of immanent importance in organic and synthetic medicinal chemistry. Its presence in “traditional” small‐molecule active pharmaceutical ingredients, in linear or cyclic oligo‐ and polypeptidic actives, including pseudopeptides, has led to the development of dedicated synthetic approaches for the formation of amide bonds starting from, if necessary, suitably protected amino acids. While the use of solid supported reagents is common in traditional peptide synthesis, similar approaches targeting amide bond formation in continuous‐flow mode took off more significantly, after a first publication in 2006, only a couple of years ago. Most efforts rely upon the transition of traditional approaches in flow mode, or the combination of solid‐phase peptide synthesis principles with flow chemistry, and advantages are mainly seen in improving space‐time yields. This Review summarizes and compares the various approaches in terms of basic amide formation, peptide synthesis, and pseudopeptide generation, describing the technological approaches and the advantages that were generated by the specific flow approaches. A final discussion highlights potential future needs and perspectives in terms of greener and more sustainable syntheses.