3-氰基-2,6-二氯-5-氟吡啶合成路线 （共 20 条）
反应条件
trichlorophosphate in (2S)-N-methyl-1-phenylpropan-2-amine hydrate; dichloromethane
反应条件
phosphorus pentachloride T=130°C; 2.5 h;
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 35, # 6 p. 2280 - 2285
反应条件
1: 90 percent / KOH / ethanol / 2 h / Ambient temperature 2: 89 percent / KF / dimethylsulfoxide / 1 h / 130 - 135 °C 3: 84 percent / conc. H2SO4 / 1 h / 50 - 55 °C View Scheme
参考文献
Miyamoto; Egawa; Shibamori; Matsumoto
Journal of Heterocyclic Chemistry, 1987 , vol. 24, # 5 p. 1333 - 1339
反应条件
1.1: sulfuric acid / 1 h / 60 - 65 °C 1.2: 20 °C / Cooling 2.1: zinc; acetic acid / methanol / 24 h / Reflux 3.1: triethylamine; trifluoroacetic anhydride / dichloromethane / 1.5 h / 0 °C View Scheme
参考文献
BAYER INTELLECTUAL PROPERTY GMBH; Follmann, Markus; Stasch, Johannes-Peter; Redlich, Gorden; Ackerstaff, Jens; Griebenow, Nils; Knorr, Andreas; Wunder, Frank; Li, Volkhart Min-Jian
Patent: US2013/172372 A1, 2013 ;
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
Miyamoto; Egawa; Matsumoto
Chemical and Pharmaceutical Bulletin, 1987 , vol. 35, # 6 p. 2280 - 2285
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
Lee, Jae Hoon; Choi, Bo Seung; Chang, Jay Hyok; Kim, Sam Sik; Shin, Hyunik
Organic Process Research and Development, 2007 , vol. 11, # 6 p. 1062 - 1064
反应条件
potassium fluoride in dimethyl sulfoxide T=20 - 130°C; 0.916667 h;
参考文献
Kreutter, Kevin; Lu, Tianbao; Lee, Yu Kai; Teleha, Christopher; Player, Mark; Zhu, Xizhen
Patent: US2006/241148 A1, 2006 ;
Location in patent: Page/Page column 12 ;
US 20060241148 A1
反应条件
1: With zinc(II) chloride in 1,2-dichloro-ethane Heating / reflux; 2: With hydrogenchloride; water in 1,2-dichloro-ethane T=90°C; 4 h; Product distribution / selectivity;
参考文献
LG LIFE SCIENCES LTD.
Patent: WO2007/64077 A1, 2007 ;
Location in patent: Page/Page column 7 ;
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 3: 1.) Mg, CCl4, EtOH / 1.) Et2O, reflux, 30 min, 2.) 10 min 4: p-toluenesulfonic acid / H2O / 2 h / Heating View Scheme
参考文献
Miyamoto; Matsumoto
Chemical and Pharmaceutical Bulletin, 1990 , vol. 38, # 12 p. 3211 - 3217
