5-叔丁氧基羰基氨基-2-氟异烟酸合成路线 （共 14 条）
反应条件
1.1: methanol; CHCl3; hexane / 2 h / 0 - 20 °C 2.1: n-BuLi / tetrahydrofuran / 1 h / -78 °C 2.2: AcOH / tetrahydrofuran / -78 - 20 °C 3.1: dimethylformamide / 5 h / 20 °C 4.1: 70 percent / (COCl)2; DMF / CH2Cl2 / 2 h / Heating View Scheme
参考文献
Wissner, Allan; Hamann, Philip R.; Nilakantan, Ramaswamy; Greenberger, Lee M.; Ye, Fei; Rapuano, Timothy A.; Loganzo, Frank
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1411 - 1416
反应条件
1.1: methanol; CHCl3; hexane / 2 h / 0 - 20 °C 2.1: n-BuLi / tetrahydrofuran / 1 h / -78 °C 2.2: AcOH / tetrahydrofuran / -78 - 20 °C 3.1: dimethylformamide / 5 h / 20 °C 4.1: 70 percent / (COCl)2; DMF / CH2Cl2 / 2 h / Heating 5.1: ethanol / 8 h / Heating View Scheme
参考文献
Wissner, Allan; Hamann, Philip R.; Nilakantan, Ramaswamy; Greenberger, Lee M.; Ye, Fei; Rapuano, Timothy A.; Loganzo, Frank
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1411 - 1416
反应条件
1.1: methanol; CHCl3; hexane / 2 h / 0 - 20 °C 2.1: n-BuLi / tetrahydrofuran / 1 h / -78 °C 2.2: AcOH / tetrahydrofuran / -78 - 20 °C 3.1: dimethylformamide / 5 h / 20 °C View Scheme
参考文献
Wissner, Allan; Hamann, Philip R.; Nilakantan, Ramaswamy; Greenberger, Lee M.; Ye, Fei; Rapuano, Timothy A.; Loganzo, Frank
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1411 - 1416
反应条件
n-butyllithium in methanol; hexane; chloroform T=0 - 20°C;
参考文献
American Cyanamid Company
Patent: US6355636 B1, 2002 ;
Location in patent: Page column 65 ;
US 6355636 B1
反应条件
in methanol; hexane; chloroform T=0 - 20°C; 2 h;
参考文献
Wyeth Holdings Corporation
Patent: EP1171440 B1, 2004 ;
Location in patent: Page 53-54 ;
反应条件
water; trifluoroacetic acid in dichloromethane 14 h; Ambient temperature;
参考文献
Rewcastle, Gordon W.; Denny, William A.; Winters, R. Thomas; Colbry, Norman L.; Showalter, H. D. Hollis
Journal of the Chemical Society - Perkin Transactions 1, 1996 , # 18 p. 2221 - 2226
反应条件
1: 94 percent / H2O, TFA / CH2Cl2 / 14 h / Ambient temperature 2: 89 percent / 2-methoxy-ethanol / 12 h / Heating View Scheme
参考文献
Rewcastle, Gordon W.; Denny, William A.; Winters, R. Thomas; Colbry, Norman L.; Showalter, H. D. Hollis
Journal of the Chemical Society - Perkin Transactions 1, 1996 , # 18 p. 2221 - 2226
参考文献
Warner-Lambert Company
Patent: US5654307 A1, 1997 ;
US 5654307 A
反应条件
1: (6-fluoro-pyridin-3-yl)-carbamic acid, tert-butyl ester With n-butyllithium; N,N,N',N,-tetramethylethylenediamine in hexane
T=-15 - -10°C; 3 h;
2: carbon dioxide in hexane
T=-70°C; 2 h;
参考文献
Zhang, Yinsheng; Huang, Yun; Huang, Che C.
Journal of Labelled Compounds and Radiopharmaceuticals, 2005 , vol. 48, # 7 p. 485 - 496
反应条件
1.1: 70 percent / H2 / Raney Ni / ethyl acetate
2.1: 96 percent / 2-methyl-propan-2-ol / 4 h / 40 °C
3.1: n-BuLi; tetramethylethylenediamine / diethyl ether / -78 °C
3.2: diethyl ether
View Scheme
参考文献
Wissner, Allan; Hamann, Philip R.; Nilakantan, Ramaswamy; Greenberger, Lee M.; Ye, Fei; Rapuano, Timothy A.; Loganzo, Frank
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1411 - 1416
