Coupling Methods: Solid-Phase Formation of Amide and Ester Bonds

The formation of amides (Fig. I) is a key step in the construction (synthesis) of natural organic compounds as well as in de novo design [1]. The amide bond is present in peptides (peptide bond), peptoids, oligocarbamates, oligoamides, and f3-lactams as well as many compounds containing rigid scaffolds such as diketopiperazines, benzodiazepines, and hydantoins. Furthermore, compounds containing amide bonds are excellent precursors for the preparation of heterocyclic compounds [2] (see Chapter 15). Thus, amide bonds play an important role in the synthesis of a majority of the compounds of biological interest.