9-溴-7-甲基-2-(4-吗啉基)-4H-吡啶并[1,2-a]嘧啶-4-酮合成路线 (共 7 条)
反应条件
1: 9-bromo-2-hydroxy-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one hydrochloride With triethylamine in tetrahydrofuran T=5°C; 0.166667 h; 2: With methanesulfonyl chloride in tetrahydrofuran T=5°C; 3: morpholine in tetrahydrofuran; water T=20 - 65°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
反应条件
1: 9-bromo-2-hydroxy-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one With trichlorophosphate 18 h; Heating; 2: morpholine in ethanol 1 h; Heating;
参考文献
Knight, Zachary A.; Chiang, Gary G.; Alaimo, Peter J.; Kenski, Denise M.; Ho, Caroline B.; Coan, Kristin; Abraham, Robert T.; Shokat, Kevan M.
Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 17 p. 4749 - 4759
反应条件
1.1: 12.7 percent / 3.5 h / 200 °C 2.1: POCl3 / 18 h / Heating 2.2: 38.8 percent / ethanol / 1 h / Heating View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 12, # 17 p. 4749 - 4759
反应条件
1: triethylamine / dichloromethane / 1 h / 22 °C 2: dichloromethane / 24 h / Reflux View Scheme
参考文献
Molecular Pharmaceutics, , vol. 9, # 6 p. 1705 - 1716
反应条件
in dichloromethane 24 h; Reflux;
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
1.1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; N-ethyl-N,N-diisopropylamine 1.2: 20 °C 2.1: toluene / 4 h / Reflux; Molecular sieve; Inert atmosphere 3.1: sodium tetrahydroborate / methanol / 1 h / 0 - 20 °C View Scheme
参考文献
Molecular Pharmaceutics, , vol. 8, # 3 p. 901 - 912
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