7,8-二甲氧基-1,3,4,5-四氢苯并氮杂卓-2-酮合成路线 （共 23 条）
反应条件
1: 95 percent / Na; liq. NH3 / tetrahydrofuran / 0.5 h / -78 °C 2: 98 percent / Me3SiCl; NaI / acetonitrile / 24 h / 20 °C View Scheme
参考文献
Tetrahedron Letters, , vol. 44, # 22 p. 4203 - 4206
反应条件
1: 71 percent / aq. silver nitrate / acetonitrile; H2O / 16 h / 20 °C 2: 95 percent / Na; liq. NH3 / tetrahydrofuran / 0.5 h / -78 °C 3: 98 percent / Me3SiCl; NaI / acetonitrile / 24 h / 20 °C View Scheme
参考文献
Tetrahedron Letters, , vol. 44, # 22 p. 4203 - 4206
反应条件
1: 63 percent / Na2CO3 / light petroleum / 15 h 2: 6.5 percent / benzene / 10 h / Ambient temperature; Irradiation View Scheme
参考文献
Heterocycles, , vol. 41, # 5 p. 959 - 972
反应条件
1: 89 percent / NaIO4 / methanol; H2O / 0 deg C to room temp. overnight 2: 12 percent / toluene-p-sulphonic acid / benzene / 0.17 h / Heating; separated to isomers 3: 84 percent / Raney nickel W-2 / ethanol / 1 h / Heating View Scheme
参考文献
Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , p. 605 - 610
反应条件
1: 12 percent / toluene-p-sulphonic acid / benzene / 0.17 h / Heating; separated to isomers 2: 84 percent / Raney nickel W-2 / ethanol / 1 h / Heating View Scheme
参考文献
Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , p. 605 - 610
反应条件
in benzene 10 h; Ambient temperatureIrradiation;
参考文献
Heterocycles, , vol. 41, # 5 p. 959 - 972
反应条件
borane in tetrahydrofuran T=70°C;
参考文献
Dalence-Guzman, Maria F.; Berglund, Magnus; Skogvall, Staffan; Sterner, Olov
Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 5 p. 2499 - 2512
反应条件
1: 7,8-dimethoxy-2-oxo-2,3,4,5-tetrahydro-1H-3-benzazepine With potassium tert-butylate in dimethyl sulfoxide T=20°C; 1 h; 2: 3-chloro-N-{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}-N-methyl-1-propanamine in dimethyl sulfoxide T=20°C; Product distribution / selectivity;
参考文献
LES LABORATOIRES SERVIER
Patent: US2012/172589 A1, 2012 ;
Location in patent: Page/Page column 3 ;
反应条件
1: 7,8-dimethoxy-2-oxo-2,3,4,5-tetrahydro-1H-3-benzazepine With potassium tert-butylate in dimethyl sulfoxide 1.08333 h; Inert atmosphere; 2: 3-chloro-N-{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}-N-methyl-1-propanamine in dimethyl sulfoxide T=25 - 30°C; 3: With hydrogenchloride in isopropyl alcohol; acetonitrile T=15 - 20°C; pH=1 - 2; 12 h; Inert atmosphere;
参考文献
Cadila Healthcare Limited
Patent: EP2097383 B1, 2012 ;
Location in patent: Page/Page column 8 ;
反应条件
sodium borohydride in 1,4-dioxane; water; acetic acid
参考文献
SCHERING CORPORATION
Patent: WO2009/14637 A2, 2009 ;
Location in patent: Page/Page column 87-88 ;
WO 2009/014637 A2
