7-溴-1,2,3,4-四氢异喹啉合成路线 （共 16 条）
反应条件
water; sodium carbonate in methanol T=60°C; 1 h;
参考文献
NOVARTIS AG
Patent: WO2008/76954 A2, 2008 ;
Location in patent: Page/Page column 51 ;
WO 2008/076954 A2
反应条件
1: in sulfuric acid; acetic acid T=20°C; 17 h; 2: With potassium carbonate in ethanol; water 1 h; Heating / reflux;
参考文献
MERCK and CO., INC.; MERCK SHARP and DOHME LIMITED
Patent: WO2004/94371 A2, 2004 ;
Location in patent: Page 81 ;
WO 2004/094371 A2
反应条件
trifluoroacetic acid in dimethyl sulfoxide T=20°C;
参考文献
WO2003/93231 A2, ;
Page/Page column 89-90 ;
WO 03/093231 A2
反应条件
1: 77 percent / CuBr, NaOMe / 24 h / 70 °C 2: NaOH / methanol; H2O / 3 h / Ambient temperature 3: ethyl acetate / 6 h / 65 °C 4: 76 percent / NaBH4, BF3*Et2O / tetrahydrofuran / 16 h / 25 °C 5: Et3N / CH2Cl2 / 0.5 h / below 0 deg C 6: NH3 / tetrahydrofuran / 60 h / -78 - 24 °C / 6205.8 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 63, # 12 p. 4116 - 4119
反应条件
1: 76 percent / NaBH4, BF3*Et2O / tetrahydrofuran / 16 h / 25 °C 2: Et3N / CH2Cl2 / 0.5 h / below 0 deg C 3: NH3 / tetrahydrofuran / 60 h / -78 - 24 °C / 6205.8 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 63, # 12 p. 4116 - 4119
反应条件
1: Et3N / CH2Cl2 / 0.5 h / below 0 deg C 2: NH3 / tetrahydrofuran / 60 h / -78 - 24 °C / 6205.8 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 63, # 12 p. 4116 - 4119
反应条件
1: NaOH / methanol; H2O / 3 h / Ambient temperature 2: ethyl acetate / 6 h / 65 °C 3: 76 percent / NaBH4, BF3*Et2O / tetrahydrofuran / 16 h / 25 °C 4: Et3N / CH2Cl2 / 0.5 h / below 0 deg C 5: NH3 / tetrahydrofuran / 60 h / -78 - 24 °C / 6205.8 Torr View Scheme
参考文献
Journal of Organic Chemistry, , vol. 63, # 12 p. 4116 - 4119
反应条件
hydrogen bromide; copper(I) bromide; sodium nitrite 2.) 75-80 deg C, 1.5 h; Yield givenMultistep reaction;
参考文献
Journal of Medicinal Chemistry, , vol. 42, # 1 p. 118 - 134
反应条件
1: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 90 °C / Inert atmosphere 2: hydrogenchloride / water / Reflux View Scheme
参考文献
REMPEX PHARMACEUTICALS, INC.; GLINKA, Tomasz; HIGUCHI, Robert; HECKER, Scott; EASTMAN, Brian; RODNY, Olga
Patent: WO2012/109164 A1, 2012 ;
WO 2012/109164 A1
