2,6-二氯-5-氟烟酸合成路线 （共 34 条）
反应条件
hydrogenchloride; trifluoroacetic acid 24 h; Heating;
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
hydrogenchloride; sodium hydroxide; lithium chloride; trichlorophosphate in dichloromethane; water
反应条件
sulfuric acid 1.) 65-75 deg C, 1 h, 2.) H2O, 100-110 deg C, 1.5 h; Yield given. Multistep reaction;
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 38, # 12 p. 3211 - 3217
反应条件
hydrogenchloride T=135 - 140°C; 3 h;
参考文献
Miyamoto; Matsumoto
Chemical and Pharmaceutical Bulletin, 1990 , vol. 38, # 12 p. 3211 - 3217
反应条件
1: thionyl chloride / 2 h / 80 °C 2: 1.) n-BuLi, biquinoline / 1.) THF, hexane, from -30 deg C to -5 deg C, 2.) THF, hexane, RT, 1 h 3: 1.) Ac2O / 1.) 130 deg C, 1 h, 2.) CH2Cl2, RT, 0.5 h 4: 59.6 percent / NaH / tetrahydrofuran / 1 h / Heating 5: 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: thionyl chloride / 2.5 h / 85 °C 2.1: 2,2'-biquinoline; n-butyllithium / tetrahydrofuran; hexane / 1 h / -50 - 20 °C 3.1: acetic anhydride / 1 h / 130 °C 3.2: 1 h 4.1: sodium hydride / tetrahydrofuran / 1.5 h / |Inert atmosphere; |Reflux 5.1: acetic acid; hydrogenchloride / 7.5 h / |Reflux View Scheme
反应条件
formic acid; triethylamine; triphenylphosphine; palladium diacetate in N,N-dimethyl-formamide T=50°C; 24 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2008/112642 A1, 2008 ;
Location in patent: Page/Page column 50; 50-51 ;
WO 2008/112642 A1
反应条件
hydrogen; triethylamine; 5 palladium over charcoal in methanol T=0 - 20°C; 4 h;
参考文献
ASAHI GLASS COMPANY, LIMITED
Patent: US2006/58529 A1, 2006 ;
Location in patent: Page/Page column 8 ;
