3-氨基-5-三氟甲基-吡啶-2-羧酸甲酯合成路线 (共 7 条)
反应条件
1: With methanol; sodium hydroxide T=20°C; 0.0166667 h; 2: With hydrogenchloride in methanol; water pH=1;
参考文献
NOVARTIS AG
Patent: US2011/230483 A1, 2011 ;
Location in patent: Page/Page column 36 ;
反应条件
1: 3-nitro-5-trifluoromethyl-pyridine-2-carbonitrile With palladium 10 on activated carbon; hydrogen in ethyl acetate
18 h;
2: With hydrogenchloride; water
24 h; Reflux;
3: methanol With sulfuric acid
84 h; Reflux;
参考文献
NOVARTIS AG; BALA, Kamlesh, Jagdis; BUTLER, Rebecca; COLLINGWOOD, Stephen, Paul; HALL, Edward, Charles; EDWARDS, Lee; LEGRAND, Darren, Mark; SPIEGEL, Katrin
Patent: WO2013/38386 A1, 2013 ;
Location in patent: Page/Page column 81 ;
反应条件
1: With sulfuric acid
48 h; Reflux;
2: With sodium hydrogencarbonate in methanol; water
T=20°C;
参考文献
NOVARTIS AG
Patent: US2011/230483 A1, 2011 ;
Location in patent: Page/Page column 32 ;
反应条件
1.1: phosphorus oxytribromide / acetonitrile / 20 °C / Reflux
2.1: tetrabutylammomium bromide / toluene / 10 h / Reflux
3.1: hydrogen / palladium 10 on activated carbon / ethyl acetate / 18 h / Inert atmosphere
4.1: hydrogenchloride; water / 24 h / Reflux
5.1: sulfuric acid / 48 h / Reflux
5.2: 20 °C
View Scheme
参考文献
NOVARTIS AG
Patent: US2011/230483 A1, 2011 ;
反应条件
1.1: tetrabutylammomium bromide / toluene / 10 h / Reflux
2.1: hydrogen / palladium 10 on activated carbon / ethyl acetate / 18 h / Inert atmosphere
3.1: hydrogenchloride; water / 24 h / Reflux
4.1: sulfuric acid / 48 h / Reflux
4.2: 20 °C
View Scheme
参考文献
NOVARTIS AG
Patent: US2011/230483 A1, 2011 ;
反应条件
1.1: hydrogen / palladium 10 on activated carbon / ethyl acetate / 18 h / Inert atmosphere
2.1: hydrogenchloride; water / 24 h / Reflux
3.1: sulfuric acid / 48 h / Reflux
3.2: 20 °C
View Scheme
参考文献
NOVARTIS AG
Patent: US2011/230483 A1, 2011 ;
反应条件
1: With sulfuric acid; bromine; acetic acid in water
T=20°C; 20 h;
2: With sodium hydrogencarbonate in water
参考文献
NOVARTIS AG; LEGRAND, Darren Mark
Patent: WO2013/38373 A1, 2013 ;
Location in patent: Page/Page column 53 ;