2,6-二氯-5-氟代烟酰氯合成路线 （共 23 条）
反应条件
thionyl chloride in toluene 3 h;
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
thionyl chloride; trichlorophosphate
参考文献
Warner-Lambert Company
Patent: US5204478 A1, 1993 ;
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
Journal of Medicinal Chemistry, , vol. 29, # 11 p. 2364 - 2369
反应条件
1: 1.) conc. H2SO4 / 1.) 65-75 deg C, 1 h, 2.) H2O, 100-110 deg C, 1.5 h 2: 81 percent / SOCl2 / 1 h / Heating View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 38, # 12 p. 3211 - 3217
反应条件
1: 81 percent / 35percent HCl / 3 h / 135 - 140 °C 2: 81 percent / SOCl2 / 1 h / Heating View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 38, # 12 p. 3211 - 3217
反应条件
1: 1.) n-BuLi, biquinoline / 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h 2: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 3: 59.6 percent / NaH / tetrahydrofuran / 1 h / Heating 4: 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: 2,2'-biquinoline; n-butyllithium / tetrahydrofuran; hexane / 1 h / -50 - 20 °C 2.1: acetic anhydride / 1 h / 130 °C 2.2: 1 h 3.1: sodium hydride / tetrahydrofuran / 1.5 h / |Inert atmosphere; |Reflux 4.1: acetic acid; hydrogenchloride / 7.5 h / |Reflux View Scheme
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
n-butyllithium; biquinoline 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h; Yield given. Multistep reaction;
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
