Recent Advances on the Synthesis of Azepane‐Based Compounds

Azepane–based compounds are saturated seven-membered carbocycles where one carbon atom is replaced with a nitrogen atom. The azepane structure is also found in fused-ring derivatives endowed of a wide range of pharmacological activities. The azepane motif is in the top 100 most frequently used ring systems for small molecule drugs. Several synthetic methods toward the preparation of new azepane-based compounds scaffolds have gained significant interest and represent a continuous challenge for synthetic organic chemists. The synthesis of the azepane ring is based on different synthetic approaches such as: ring-closing reactions; ring-expansion reactions of cyclic compounds; and multistep sequences. The azepane based compounds continue to play great synthetic relevance because of their different biological activities such as anti-cancer, antimicrobial, anti-Alzheimer's disease and anticonvulsant activity. New synthetic methods for the construction of azepane derivatives endowed of relevant biological activity and good pharmacological profiles is expected in near future.