3 - [（3 -氨基- 4 -甲基苯甲酰）吡啶-2基氨基]丙酸乙酯合成路线 （共 14 条）
反应条件
hydrogen; palladium 10 on activated carbon in ethyl acetate T=50°C; P=2250.23 - 3000.3 Torr; 4 - 5 h; Product distribution / selectivity;
参考文献
WO2007/71742 A1, ;
Page/Page column 22-23 ;
反应条件
sodium dithionite in ethanol; water T=50°C;
参考文献
WO2009/111997 A1, ;
Page/Page column 10-11 ;
反应条件
1: SOCl2 / dimethylformamide / 0.5 h / Heating 2: Et3N / tetrahydrofuran / 20 °C 3: 65 percent / H2 / 10percent Pd/C / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 45, # 9 p. 1757 - 1766
反应条件
1: Et3N / tetrahydrofuran / 20 °C 2: 65 percent / H2 / 10percent Pd/C / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 45, # 9 p. 1757 - 1766
反应条件
1.1: thionyl chloride / N,N-dimethyl-formamide / 0.75 h / Reflux 2.1: triethylamine / tetrahydrofuran / 0 - 20 °C 2.2: 1.5 h / 0 - 20 °C 3.1: sodium hydroxide / dichloromethane; water 3.2: 55 °C / 3000.3 Torr View Scheme
反应条件
1.1: 25 - 55 °C 2.1: thionyl chloride / N,N-dimethyl-formamide / 1.25 h / 25 - 80 °C 2.2: 1 h 3.1: palladium on activated charcoal / ethyl acetate / 0.33 h / 25 - 55 °C / |High pressure View Scheme
反应条件
1.1: ethyl acetate / 2 h / 20 - 65 °C 1.2: 0.75 h / 40 °C 2.1: sodium hydroxide / water; acetic acid n-butyl ester / 50 °C 2.2: 2 h / 40 °C 3.1: acetone / 6 h / 0 - 33 °C / Reflux View Scheme
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Patent: US2011/275824 A1, 2011 ;
反应条件
1.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 0.75 h / Inert atmosphere; Reflux 1.2: 6 h / Reflux 1.3: 1 h / Reflux 2.1: hydrogenchloride / isopropyl alcohol / 1 h / 0 - 35 °C 3.1: hydrogenchloride / 24 h / 30 °C 4.1: (NH4)2CO3 / ethanol / 20 °C / Inert atmosphere 5.1: triethylamine / acetone / 1.5 h / 0 - 20 °C / Inert atmosphere View Scheme
反应条件
toluene-4-sulfonic acid in ethyl acetate T=20 - 60°C; 3 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Patent: US2011/275824 A1, 2011 ;
Location in patent: Page/Page column 5 ;
反应条件
1: in ethyl acetate T=20 - 65°C; 2 h; 2: With potassium carbonate in ethyl acetate T=40°C; 0.75 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Patent: US2011/275824 A1, 2011 ;
Location in patent: Page/Page column 5 ;
