title: Synthesis of Substituted 2,3-Benzodiazepines.
abstract: A new, four-step synthetic route for substituted 2,3-benzodiazepines 1, starting from aldehyde 4, was developed with excellent overall yields. This route included the 1,2-addition of various aromatic Grignard reagents to 4, PCC oxidation, and aerobic Wacker-type oxidation of the olefinic group of 6, followed by condensation of the resulting 1,5-dicarbonyl 7 with N2H4. Isoquinolones 9 were obtained when an aldehyde group was used instead of a ketone. The key structures were confirmed by X-ray single-crystal diffraction analysis.
authors.affiliation: Department of Medicinal and Applied Chemistry and General Research Centers of R&D Office, Kaohsiung Medical University , Kaohsiung 807, Taiwan.
authors.forename: Chieh-Kai
authors.initials: CK
authors.lastname: Chan
authors.affiliation: Department of Medicinal and Applied Chemistry and General Research Centers of R&D Office, Kaohsiung Medical University , Kaohsiung 807, Taiwan.
authors.forename: Yu-Lin
authors.initials: YL
authors.lastname: Tsai
authors.affiliation: Department of Medicinal and Applied Chemistry and General Research Centers of R&D Office, Kaohsiung Medical University , Kaohsiung 807, Taiwan.
authors.forename: Yi-Ling
authors.initials: YL
authors.lastname: Chan
authors.affiliation: Department of Medicinal and Applied Chemistry and General Research Centers of R&D Office, Kaohsiung Medical University , Kaohsiung 807, Taiwan.
authors.forename: Meng-Yang
authors.initials: MY
authors.lastname: Chang