9-(1-羟基乙基)-7-甲基-2-(吗啉-4-基)-4H-吡啶并[1,2-a]嘧啶-4-酮合成路线 (共 5 条)
反应条件
1: dichloromethane / 48 h / 22 °C 2: triethylamine / dichloromethane / 1 h / 22 °C 3: dichloromethane / 24 h / Reflux 4: palladium(II) dichloride bis[bis(diphenylphosphine)ferrocene]; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 16.5 h / 22 - 120 °C / Inert atmosphere 5: hydrogenchloride; water / N,N-dimethyl-formamide / 22 °C 6: sodium tetrahydroborate / methanol; dichloromethane / 0 - 22 °C View Scheme
参考文献
Zhao, Yunqi; Duan, Shaofeng; Zeng, Xing; Liu, Chunjing; Davies, Neal M.; Li, Benyi; Forrest, M. Laird
Molecular Pharmaceutics, 2012 , vol. 9, # 6 p. 1705 - 1716
反应条件
1: triethylamine / dichloromethane / 1 h / 22 °C 2: dichloromethane / 24 h / Reflux 3: palladium(II) dichloride bis[bis(diphenylphosphine)ferrocene]; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 16.5 h / 22 - 120 °C / Inert atmosphere 4: hydrogenchloride; water / N,N-dimethyl-formamide / 22 °C 5: sodium tetrahydroborate / methanol; dichloromethane / 0 - 22 °C View Scheme
参考文献
Zhao, Yunqi; Duan, Shaofeng; Zeng, Xing; Liu, Chunjing; Davies, Neal M.; Li, Benyi; Forrest, M. Laird
Molecular Pharmaceutics, 2012 , vol. 9, # 6 p. 1705 - 1716
反应条件
1: palladium(II) dichloride bis[bis(diphenylphosphine)ferrocene]; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 16.5 h / 22 - 120 °C / Inert atmosphere 2: hydrogenchloride; water / N,N-dimethyl-formamide / 22 °C 3: sodium tetrahydroborate / methanol; dichloromethane / 0 - 22 °C View Scheme
参考文献
Zhao, Yunqi; Duan, Shaofeng; Zeng, Xing; Liu, Chunjing; Davies, Neal M.; Li, Benyi; Forrest, M. Laird
Molecular Pharmaceutics, 2012 , vol. 9, # 6 p. 1705 - 1716
反应条件
1: triethylamine / dichloromethane / 0 - 22 °C 2: triethylamine / Reflux View Scheme
参考文献
Molecular Pharmaceutics, , vol. 9, # 6 p. 1705 - 1716
反应条件
1: 9-(1-hydroxyethyl)-7-methyl-2-morpholin-4-yl-4H-pyrido[1,2-a]pyrimidin-4-one With phosphorus tribromide in dichloromethane
T=40°C; 2.5 h;
2: anthranilic acid With triethylamine in dichloromethane
T=40°C;
3: With hydrogenchloride; water in acetone
T=20°C;
参考文献
Fjellstrom, Ola; Gustafsson, David; Lindberg, Jan A.; Jackson, Shaun
Patent: US2009/191177 A1, 2009 ;
Location in patent: Page/Page column 7 ;
US 20090191177 A1