N-Boc-5-氨基-2-氟吡啶合成路线 （共 12 条）
反应条件
in tert-butyl alcohol T=40°C; 4 h;
参考文献
Wyeth Holdings Corporation
Patent: EP1171440 B1, 2004 ;
Location in patent: Page 53 ;
反应条件
1: 70 percent / H2 / Raney Ni / ethyl acetate 2: 96 percent / 2-methyl-propan-2-ol / 4 h / 40 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 14, # 6 p. 1411 - 1416
反应条件
1: 84 percent / KF / dimethylsulfoxide / 18 h / 70 °C 2: 70 percent / H2 / Raney Ni / ethyl acetate 3: 96 percent / 2-methyl-propan-2-ol / 4 h / 40 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 14, # 6 p. 1411 - 1416
反应条件
1.1: n-BuLi; tetramethylethylenediamine / diethyl ether / -78 °C 1.2: diethyl ether 2.1: methanol; CHCl3; hexane / 2 h / 0 - 20 °C 3.1: n-BuLi / tetrahydrofuran / 1 h / -78 °C 3.2: AcOH / tetrahydrofuran / -78 - 20 °C 4.1: dimethylformamide / 5 h / 20 °C 5.1: 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: n-BuLi; tetramethylethylenediamine / diethyl ether / -78 °C 1.2: diethyl ether 2.1: methanol; CHCl3; hexane / 2 h / 0 - 20 °C 3.1: n-BuLi / tetrahydrofuran / 1 h / -78 °C 3.2: AcOH / tetrahydrofuran / -78 - 20 °C 4.1: dimethylformamide / 5 h / 20 °C 5.1: 70 percent / (COCl)2; DMF / CH2Cl2 / 2 h / Heating 6.1: 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: n-BuLi; tetramethylethylenediamine / diethyl ether / -78 °C 1.2: diethyl ether 2.1: methanol; CHCl3; hexane / 2 h / 0 - 20 °C 3.1: n-BuLi / tetrahydrofuran / 1 h / -78 °C 3.2: AcOH / tetrahydrofuran / -78 - 20 °C 4.1: 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
1.1: n-BuLi; tetramethylethylenediamine / diethyl ether / -78 °C 1.2: diethyl ether 2.1: methanol; CHCl3; hexane / 2 h / 0 - 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
1.1: n-BuLi; TMEDA / hexane; various solvent(s) / 3 h / -15 - -10 °C 1.2: 64 percent / hexane; various solvent(s) / 2 h / -70 °C 2.1: 85 percent / trifluoroacetic acid / CH2Cl2 / 3 h / 20 °C 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
反应条件
1: 47 percent / TMEDA, BuLi / diethyl ether; hexane / 1.) -40 deg C, 16 h, 2.) -40 deg C to r.t., 1 h 2: 94 percent / H2O, TFA / CH2Cl2 / 14 h / Ambient temperature 3: 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
