title: Concise synthesis of 2-benzazepine derivatives and their biological activity.
abstract: 2-Benzazepines, which are potentially good candidates for new drug therapies to treat skin wounds, were readily prepared from substituted cinnamylamide via an intramolecular Friedel-Crafts reaction. With few steps and effective reactions, the procedure enables a rapid derivatization of 2-benzazepines. Moreover, optically active 4-substituted-2-benzazepines were prepared from chiral α-substituted cinnamylamides, which were readily prepared by asymmetric α-alkylation of chiral cinnamyl oxazolidinone amides. We have easily prepared a library of more than 20 derivatives and examined the biological activity of the compounds.
authors.affiliation: Department of Applied Molecular Bioscience, Graduate School of Medicine, Yamaguchi University, Ube 755-8611, Japan.
authors.forename: Masahiro
authors.initials: M
authors.lastname: So
authors.forename: Tomoko
authors.initials: T
authors.lastname: Kotake
authors.forename: Kenji
authors.initials: K
authors.lastname: Matsuura
authors.forename: Makoto
authors.initials: M
authors.lastname: Inui
authors.forename: Akio
authors.initials: A
authors.lastname: Kamimura
mesh_terms: D000478:Alkylation; D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D003500:Cyclization; D015394:Molecular Structure; D013237:Stereoisomerism
chemical_list: D001552:Benzazepines