title: Synthesis of a 10,000 member 1,5-benzodiazepine-2-one library by the directed sorting method.
abstract: The solid-phase synthesis of a 10,000 member combinatorial library of 1,5-benzodiazepine-2-one derivatives is reported. The 3-amino-1,5-benzodiazepine-2-one scaffold was prepared in solution, and the benzamide nitrogen was used as a point of attachment to the resin. The 5-aniline and 3-amine were then used as points of diversity. A 10,000 member library was synthesized using the Irori directed sorting system, and after analysis of a representative sample from the library, the Irori system was used to remove the compounds of lower purity.
authors.affiliation: Rhône-Poulenc Rorer Research and Development, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA.
authors.forename: T F
authors.initials: TF
authors.lastname: Herpin
authors.forename: K G
authors.initials: KG
authors.lastname: Van Kirk
authors.forename: J M
authors.initials: JM
authors.lastname: Salvino
authors.forename: S T
authors.initials: ST
authors.lastname: Yu
authors.forename: R F
authors.initials: RF
authors.lastname: Labaudinière
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry; D000595:Amino Acid Sequence; D014151:Anti-Anxiety Agents / Q000737:chemistry*; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D015195:Drug Design; D004399:Dynorphins / Q000737:chemistry; D008024:Ligands; D008969:Molecular Sequence Data; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D008024:Ligands; D004399:Dynorphins