title: Multicomponent synthesis of diverse 1,4-benzodiazepine scaffolds.
abstract: The 1,4-benzodiazepine (BDZ) scaffold is of particular interest in drug design due to a balanced ensemble of beneficial physicochemical properties including a semirigid and compact diazepine ring with spatial placements of several substituents, combined with low number of rotatable bonds, hydrogen bond donors and acceptors, and intermediate lipophilicity. As an alternative to traditional multistep sequential syntheses, we designed routes employing one-pot MCRs to accelerate access diverse BDZ scaffolds in two or three steps.
authors.affiliation: Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania 15261, USA.
authors.forename: Yijun
authors.initials: Y
authors.lastname: Huang
authors.forename: Kareem
authors.initials: K
authors.lastname: Khoury
authors.forename: Tyler
authors.initials: T
authors.lastname: Chanas
authors.forename: Alexander
authors.initials: A
authors.lastname: Dömling
mesh_terms: D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D006860:Hydrogen Bonding; D008968:Molecular Conformation; D015394:Molecular Structure
chemical_list: D001569:Benzodiazepines; C468549:Bz-423