1-(2-氨基吡啶-4-基)-2-(4-氟苯基)-乙酮合成路线 （共 6 条）
反应条件
1: With water; hydrogen bromide
30 h; Heating / reflux;
2: With ammonia in water
T=0°C;
参考文献
MERCKLE GMBH
Patent: EP1894925 A1, 2008 ;
Location in patent: Page/Page column 14-15; 41 ;
反应条件
hydrogen bromide in water
30 h; Heating;
参考文献
Wagner, Gerd K.; Kotschenreuther, Dunja; Zimmermann, Werner; Laufer, Stefan A.
Journal of Organic Chemistry, 2003 , vol. 68, # 11 p. 4527 - 4530
反应条件
1.1: carbonyldiimidazole / tetrahydrofuran / 0.75 h / 20 °C
1.2: 62 percent / KOt-Bu / tetrahydrofuran / 2 h / 120 °C
2.1: 50 percent / aq. HBr / 30 h / Heating
View Scheme
参考文献
Laufer, Stefan A.; Zimmermann, Werner; Ruff, Kathrin J.
Journal of Medicinal Chemistry, 2004 , vol. 47, # 25 p. 6311 - 6325
反应条件
1.1: carbonyldiimidazole / tetrahydrofuran / 0.75 h / 20 °C
1.2: 62 percent / KOt-Bu / tetrahydrofuran / 2 h / 120 °C
2.1: 50 percent / aq. HBr / 30 h / Heating
View Scheme
参考文献
Laufer, Stefan A.; Zimmermann, Werner; Ruff, Kathrin J.
Journal of Medicinal Chemistry, 2004 , vol. 47, # 25 p. 6311 - 6325
反应条件
1.1: 75 percent / 4-dimethylaminopyridine / 5 h / Heating
2.1: 42 percent / potassium permanganate / H2O / 2.5 h / 50 - 90 °C
3.1: carbonyldiimidazole / dimethylformamide / 0.75 h / 20 °C
3.2: 65 percent / potassium tert-butoxide / dimethylformamide / 2 h / 120 °C
4.1: 55 percent / HBr / H2O / 30 h / Heating
View Scheme
参考文献
Wagner, Gerd K.; Kotschenreuther, Dunja; Zimmermann, Werner; Laufer, Stefan A.
Journal of Organic Chemistry, 2003 , vol. 68, # 11 p. 4527 - 4530
反应条件
1.1: 42 percent / potassium permanganate / H2O / 2.5 h / 50 - 90 °C
2.1: carbonyldiimidazole / dimethylformamide / 0.75 h / 20 °C
2.2: 65 percent / potassium tert-butoxide / dimethylformamide / 2 h / 120 °C
3.1: 55 percent / HBr / H2O / 30 h / Heating
View Scheme
参考文献
Wagner, Gerd K.; Kotschenreuther, Dunja; Zimmermann, Werner; Laufer, Stefan A.
Journal of Organic Chemistry, 2003 , vol. 68, # 11 p. 4527 - 4530
