2-氯-5-氟吡啶 1-氧化物合成路线 (共 8 条)
反应条件
1: 59 percent / conc. H2SO4; KNO3 / 2 h / 120 °C 2: 91 percent / H2 / Raney Ni / ethanol / 3 h / 2068.59 Torr 3: 83 percent / conc. H2SO4; KNO3 / 0 - 20 °C 4: 90 percent / conc. H2SO4 / 20 °C 5: 94 percent / H2 / Raney Ni / ethanol View Scheme
参考文献
F. HOFFMANN-LA ROCHE AG; LAI, Yingjie; LIANG, Jun; MAGNUSON, Steven R.; TSUI, Vickie H.; ZHANG, Birong; ROBARGE, Kirk
Patent: WO2011/113802 A2, 2011 ;
WO 2011/113802 A2
反应条件
1: 59 percent / conc. H2SO4; KNO3 / 2 h / 120 °C 2: 91 percent / H2 / Raney Ni / ethanol / 3 h / 2068.59 Torr 3: 83 percent / conc. H2SO4; KNO3 / 0 - 20 °C 4: 90 percent / conc. H2SO4 / 20 °C View Scheme
参考文献
F. HOFFMANN-LA ROCHE AG; LAI, Yingjie; LIANG, Jun; MAGNUSON, Steven R.; TSUI, Vickie H.; ZHANG, Birong; ROBARGE, Kirk
Patent: WO2011/113802 A2, 2011 ;
WO 2011/113802 A2
反应条件
1: 59 percent / conc. H2SO4; KNO3 / 2 h / 120 °C 2: 91 percent / H2 / Raney Ni / ethanol / 3 h / 2068.59 Torr View Scheme
参考文献
F. HOFFMANN-LA ROCHE AG; LAI, Yingjie; LIANG, Jun; MAGNUSON, Steven R.; TSUI, Vickie H.; ZHANG, Birong; ROBARGE, Kirk
Patent: WO2011/113802 A2, 2011 ;
WO 2011/113802 A2
反应条件
1.1: potassium nitrate; sulfuric acid / 2 h / 120 °C 1.2: 15 °C / Cooling with ice 2.1: hydrogen / Raney nickel / ethanol / 3 h / 2068.65 Torr 3.1: potassium nitrate; sulfuric acid / 1.17 h / 0 - 20 °C 3.2: 12 h / 20 °C 3.3: 5 °C / Cooling with ice 4.1: hydrogen / Raney nickel / ethanol / 2 h / 1861.78 Torr 5.1: oxygen; anhydrous iron chloride / 1,4-dioxane; ethanol / 10 h / 75 °C 5.2: Cooling with ice 6.1: trimethylsilyl bromide / anhydrous propionitrile / 12 h / 120 °C 6.2: 23 °C / Cooling with ice View Scheme
参考文献
F. HOFFMANN-LA ROCHE AG; LAI, Yingjie; LIANG, Jun; MAGNUSON, Steven R.; TSUI, Vickie H.; ZHANG, Birong; ROBARGE, Kirk
Patent: WO2011/113802 A2, 2011 ;
WO 2011/113802 A2
反应条件
1: With dihydrogen peroxide; trifluoroacetic acid in water
T=70 - 75°C;
2: With ammonium hydroxide in dichloromethane; water
参考文献
F. HOFFMANN-LA ROCHE AG; LAI, Yingjie; LIANG, Jun; MAGNUSON, Steven R.; TSUI, Vickie H.; ZHANG, Birong; ROBARGE, Kirk
Patent: WO2011/113802 A2, 2011 ;
Location in patent: Page/Page column 106 ;
WO 2011/113802 A2
反应条件
1: 59 percent / conc. H2SO4; KNO3 / 2 h / 120 °C
2: 91 percent / H2 / Raney Ni / ethanol / 3 h / 2068.59 Torr
3: 83 percent / conc. H2SO4; KNO3 / 0 - 20 °C
4: 90 percent / conc. H2SO4 / 20 °C
5: 94 percent / H2 / Raney Ni / ethanol
View Scheme
参考文献
Liu; Luo; Mozdziesz; Lin; Dutschman; Gullen; Cheng; Sartorelli
Nucleosides, Nucleotides and Nucleic Acids, 2001 , vol. 20, # 12 p. 1975 - 2000
反应条件
sulfuric acid; potassium nitrate
T=120°C; 2 h;
参考文献
F. HOFFMANN-LA ROCHE AG; LAI, Yingjie; LIANG, Jun; MAGNUSON, Steven R.; TSUI, Vickie H.; ZHANG, Birong; ROBARGE, Kirk
Patent: WO2011/113802 A2, 2011 ;
Location in patent: Page/Page column 106-107 ;
WO 2011/113802 A2
反应条件
1: 59 percent / conc. H2SO4; KNO3 / 2 h / 120 °C
2: 91 percent / H2 / Raney Ni / ethanol / 3 h / 2068.59 Torr
3: 83 percent / conc. H2SO4; KNO3 / 0 - 20 °C
View Scheme
参考文献
Liu; Luo; Mozdziesz; Lin; Dutschman; Gullen; Cheng; Sartorelli
Nucleosides, Nucleotides and Nucleic Acids, 2001 , vol. 20, # 12 p. 1975 - 2000