2,6-二氯-5-氟吡啶-3-羧酸乙酯合成路线 （共 22 条）
反应条件
thionyl chloride; sodium hydrogencarbonate; triethylamine in ethanol; hexane
参考文献
Abbott Laboratories
Patent: US5250548 A1, 1993 ;
US 5250548 A
反应条件
in ethanol T=0°C; 1.25 h; Heating / reflux;
参考文献
AstraZeneca AB
Patent: US2008/171732 A1, 2008 ;
Location in patent: Page/Page column 40 ;
US 20080171732 A1
反应条件
T=0°C; 1.25 h; Heating / reflux;
参考文献
ASTRAZENECA AB
Patent: WO2008/85119 A1, 2008 ;
Location in patent: Page/Page column 209 ;
WO 2008/085119 A1
反应条件
triethylamine in toluene T=0 - 20°C; 1 h;
参考文献
EP1640366 A1, ;
Page/Page column 27-28 ;
反应条件
boron trifluoride diethyl etherate in ethanol 1.) 60 deg C, 30 min; 2.) reflux, 16 h;
参考文献
Miyamoto; Egawa; Matsumoto
Chemical and Pharmaceutical Bulletin, 1987 , vol. 35, # 6 p. 2280 - 2285
反应条件
1: 84 percent / conc. H2SO4 / 1 h / 60 - 65 °C 2: 79 percent / BF3-Et2O / ethanol / 1.) 60 deg C, 30 min; 2.) reflux, 16 h View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 35, # 6 p. 2280 - 2285
反应条件
1: 77 percent / PCl5 / 2.5 h / 130 °C 2: 84 percent / conc. H2SO4 / 1 h / 60 - 65 °C 3: 79 percent / BF3-Et2O / ethanol / 1.) 60 deg C, 30 min; 2.) reflux, 16 h View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 35, # 6 p. 2280 - 2285
反应条件
1: 73.2 percent / trifluoroacetic acid, 7.5 N aq. HCl / 24 h / Heating 2: thionyl chloride / 2 h / 80 °C 3: 1.) n-BuLi, biquinoline / 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h 4: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 5: 59.6 percent / NaH / tetrahydrofuran / 1 h / Heating 6: 60 percent / pyridine / 3 h / Ambient temperature View Scheme
参考文献
Chu, Daniel T. W.; Fernandes, Prabhavathi B.; Claiborne, Akiyo K.; Gracey, Eugene H.; Pernet, Andre G.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2364 - 2369
反应条件
1.1: trifluoroacetic acid; hydrogenchloride / water / 26 h / |Reflux 2.1: thionyl chloride / 2.5 h / 85 °C 3.1: 2,2'-biquinoline; n-butyllithium / tetrahydrofuran; hexane / 1 h / -50 - 20 °C 4.1: acetic anhydride / 1 h / 130 °C 4.2: 1 h 5.1: sodium hydride / tetrahydrofuran / 1.5 h / |Inert atmosphere; |Reflux 6.1: acetic acid; hydrogenchloride / 7.5 h / |Reflux View Scheme
反应条件
1: 73.2 percent / trifluoroacetic acid, 7.5 N aq. HCl / 24 h / Heating 2: thionyl chloride / 2 h / 80 °C View Scheme
参考文献
Vymed Corporation; SHETTY, B. Vithal
Patent: US2014/73631 A1, 2014 ;
