5-溴-1H-吡咯并[2,3-b]吡啶-2-酮合成路线 （共 20 条）
反应条件
triethylamine; 1,3-bis-(diphenylphosphino)propane in ethanol; dimethyl sulfoxide T=95°C; 18 h; Heating / reflux;
参考文献
Glaxo Wellcome Inc.
Patent: US6350747 B1, 2002 ;
Location in patent: Page column 70 ;
反应条件
palladium diacetate in ethanol; dimethyl sulfoxide; triethylamine
参考文献
SmithKline Beecham Corporation
Patent: US6369086 B1, 2002 ;
US 6369086 B1
反应条件
palladium diacetate in ethanol; dimethyl sulfoxide; triethylamine
参考文献
SmithKline Beecham Corporation
Patent: US6624171 B1, 2003 ;
US 6624171 B1
反应条件
palladium diacetate; 1,4-(bisdiphenylphosphino)propane; triethylamine in dimethyl sulfoxide T=95°C; P=2068.59 Torr; 18 h;
参考文献
Cheung, Mui; Hunter, Robert N.; Peel, Michael R.; Lackey, Karen E.
Heterocycles, 2001 , vol. 55, # 8 p. 1583 - 1590
反应条件
1: 5-Bromo-1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one With sodium hydride in N,N-dimethyl-formamide T=-40°C; 1 h; Inert atmosphere; 2: methyl iodide in N,N-dimethyl-formamide T=-40°C; 2 h;
参考文献
EUROSCREEN S.A.; HOVEYDA, Hamid; DUTHEUIL, Guillaume; EL BOUSMAQUI, Mohamed; BERNARD, Jerome
Patent: WO2011/151434 A1, 2011 ;
Location in patent: Page/Page column 52-53 ;
WO 2011/151434 A1
反应条件
1: With borane-THF in tetrahydrofuran T=0 - 20°C; 0.583333 h; 2: With manganese triacetate in acetic acid T=75°C; 0.75 h;
参考文献
Wu, Pei-Wen; Hsieh, Wan-Ting; Cheng, Yi-Ming; Wei, Ching-Yen; Chou, Pi-Tai
Journal of the American Chemical Society, 2006 , vol. 128, # 45 p. 14426 - 14427
反应条件
1.1: BH3*THF / tetrahydrofuran / 0.83 h / 20 °C 1.2: 50 percent / Mn(OAc)3*2H2O; acetic acid / 0.83 h / 75 °C 2.1: 85 percent / CuBr / methanol; dimethylformamide / 3 h / Heating View Scheme
参考文献
Mazeas, Daniel; Guillaumet, Gerald; Viaud, Marie-Claude
Heterocycles, 1999 , vol. 50, # 2 p. 1065 - 1080
反应条件
copper(l) iodide; trans-N,N'-dimethylcyclohexane-1,2-diamine; sodium iodide in 1,4-dioxane T=110°C; 24 h; Inert atmosphereDarkness;
参考文献
European Journal of Medicinal Chemistry, , vol. 44, # 6 p. 2705 - 2710
反应条件
potassium acetate; 1,1'-bis-(diphenylphosphino)ferrocene; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in 1,4-dioxane T=120°C; 8 h;
参考文献
KUDOS PHARMACEUTICALS LIMITED
Patent: WO2008/23161 A1, 2008 ;
Location in patent: Page/Page column 111 ;
WO 2008/023161 A1
反应条件
1.1: borane*tetrahydrofurane / tetrahydrofuran / 0.58 h / 0 - 20 °C
1.2: 50 percent / manganese triacetate / acetic acid / 0.75 h / 75 °C
2.1: 54 percent / sodium hydride in oil / dimethylformamide / 12 h / 0 - 20 °C
View Scheme
参考文献
Guillard, Jerome; Larraya, Carlos; Viaud-Massuard, Marie-Claude
Heterocycles, 2003 , vol. 60, # 4 p. 865 - 877
