4-氯-N-甲基-2-吡啶甲酰胺合成路线 （共 18 条）
反应条件
potassium tert-butylate; potassium carbonate in N,N-dimethyl-formamide T=20 - 90°C; 1 h; Inert atmosphere;
参考文献
Yao, Jianwen; He, Zuopeng; Chen, Jing; Sun, Wei; Fang, Hao; Xu, Wenfang
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 21 p. 6549 - 6553,5
反应条件
hydrogenchloride in water; acetone T=5 - 40°C; 1 h;
参考文献
WO2006/34796 A1, ;
Page/Page column 17 ;
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
BAYER PHARMACEUTICALS CORPORATION
Patent: WO2005/9961 A2, 2005 ;
Location in patent: 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
BAYER PHARMA AKTIENGESELLSCHAFT; STIEHL, Juergen; HEILMANN, Werner; LOeGERS, Michael; REHSE, Joachim; GOTTFRIED, Michael; WICHMANN, Saskia
Patent: WO2011/128261 A1, 2011 ;
Location in patent: 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
BAYER PHARMA AKTIENGESELLSCHAFT; STIEHL, Juergen; HEILMANN, Werner; LOeGERS, Michael; REHSE, Joachim; GOTTFRIED, Michael; WICHMANN, Saskia
Patent: WO2011/128261 A1, 2011 ;
Location in patent: 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
BAYER PHARMA AKTIENGESELLSCHAFT; STIEHL, Juergen; HEILMANN, Werner; LOeGERS, Michael; REHSE, Joachim; GOTTFRIED, Michael; WICHMANN, Saskia
Patent: WO2011/128261 A1, 2011 ;
Location in patent: Page/Page column 16-17 ;
反应条件
1: 1-(4-chloro-3-(trifluromethyl)phenyl)-3-(4-hydroxyphenyl)urea With potassium tert-butylate in N,N-dimethyl-formamide T=20°C; 2 - 3 h; 2: 4-chloro-N-methyl-2-pyridinecarboxamide in N,N-dimethyl-formamide T=60 - 70°C; 2 - 3 h; Product distribution / selectivity;
参考文献
CIPLA LIMITED
Patent: US2010/311980 A1, 2010 ;
Location in patent: Page/Page column 21 ;
反应条件
1: potassium tert-butylate; potassium carbonate / N,N-dimethyl-formamide 2: dichloromethane / 22 h / 0 °C View Scheme
参考文献
Bankston, Donald; Dumas, Jacques; Natero, Reina; Riedl, Bernd; Monahan, Mary-Katherine; Sibley, Robert
Organic Process Research and Development, 2002 , vol. 6, # 6 p. 777 - 781
反应条件
potassium tert-butylate in N,N-dimethyl-formamide T=25°C; 1 h;
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 21, # 8 p. 2220 - 2223
