4-(4-氨基-3-氟苯氧基)-N-甲基吡啶-2-甲酰胺合成路线 （共 11 条）
反应条件
1: 2-fluoro-4-hydroxyaniline With potassium tert-butylate in DMA T=20°C; 0.5 h; Sonographic reaction; 2: 4-chloro-N-methyl-2-pyridinecarboxamide in DMA T=100°C;
参考文献
DECIPHERA PHARMACEUTICALS, LLC; FLYNN, Daniel L.; PETILLO, Peter A.; KAUFMAN, Michael D.
Patent: WO2013/36232 A2, 2013 ;
Location in patent: Paragraph 00220 ;
反应条件
1: 2-fluoro-4-hydroxyaniline With potassium tert-butylate in isobutyramide T=0°C; 0.416667 h; 2: 4-chloro-N-methyl-2-pyridinecarboxamide in isobutyramide T=100°C; 16 h;
参考文献
WO2005/9961 A2, ;
Page/Page column 46-47 ;
WO 2005/009961 A2
反应条件
1: in 1-methyl-pyrrolidin-2-one T=100°C; 2: With potassium tert-butylate in tetrahydrofuran; 1-methyl-pyrrolidin-2-one T=100°C; 4.16667 h; 3: With acetic acid in tetrahydrofuran; 1-methyl-pyrrolidin-2-one; water; toluene T=80°C; 0.166667 h;
参考文献
WO2011/128261 A1, ;
Page/Page column 15-16 ;
反应条件
1: in 1-methyl-pyrrolidin-2-one T=100°C; 2: With potassium tert-butylate in tetrahydrofuran; 1-methyl-pyrrolidin-2-one T=100°C; 5.5 h; 3: With acetic acid in tetrahydrofuran; 1-methyl-pyrrolidin-2-one; water; toluene T=80°C; 0.166667 h;
参考文献
WO2011/128261 A1, ;
Page/Page column 15-16 ;
反应条件
1: in 1-methyl-pyrrolidin-2-one T=100°C; 2: With potassium tert-butylate in tetrahydrofuran; 1-methyl-pyrrolidin-2-one T=100°C; 3.66667 h; 3: With acetic acid in tetrahydrofuran; 1-methyl-pyrrolidin-2-one; water; toluene T=80°C; 0.166667 h;
参考文献
WO2011/128261 A1, ;
Page/Page column 16-17 ;
反应条件
1.1: hydrogen / palladium 10 on activated carbon / ethyl acetate / 4 h 2.1: potassium tert-butylate / N,N-dimethyl acetamide / 0.42 h / 0 °C 2.2: 16 h / 100 °C View Scheme
参考文献
WO2011/130728 A1, ;
WO 2011/130728 A1
反应条件
1.1: ethanol; tetrahydrofuran / 4 h / 0 - 3 °C 2.1: potassium tert-butylate / N,N-dimethyl acetamide / 0.5 h / 20 °C / |Inert atmosphere 2.2: 100 °C / |Inert atmosphere View Scheme
反应条件
1.1: Reflux 2.1: 1-methyl-pyrrolidin-2-one / 100 °C 2.2: 4.17 h / 100 °C 2.3: 0.17 h / 80 °C View Scheme
反应条件
1: toluene / 72 h / 20 °C 2: hydrogenchloride / 1,4-dioxane; tetrahydrofuran View Scheme
参考文献
BAYER HEALTHCARE LLC; WILHELM, Scott
Patent: WO2011/130728 A1, 2011 ;
WO 2011/130728 A1
反应条件
in toluene T=20°C; 72 h;
参考文献
WO2005/9961 A2, ;
Page/Page column 47 ;
WO 2005/009961 A2
