4-溴-2,6-二氟苯胺合成路线 (共 12 条)
反应条件
1: With bromine; acetic acid in water T=20°C; 0.25 h; 2: With sodium carbonate in water
参考文献
JANSSEN PHARMACEUTICA N.V.; ARTS, Frank, Xavier, Jozef, Herwig
Patent: WO2006/15985 A1, 2006 ;
Location in patent: Page/Page column 54 ;
反应条件
bromine in chloroform
反应条件
1: With 1,3-bis-(diphenylphosphino)propane; potassium carbonate; palladium diacetate in DMF (N,N-dimethyl-formamide); water T=20 - 80°C; 24 h; 2: With formic acid; water in acetonitrile T=20°C; 0.75 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2004/110997 A1, 2004 ;
Location in patent: Page 52-53 ;
WO 2004/110997 A1
反应条件
n-butyllithium T=-60 - -50°C;
参考文献
Asato, Goro; Baker, Pamela K.; Bass, Roy T.; Bentley, T. James; Chari, Sarangan; et al.
Agricultural and Biological Chemistry, 1984 , vol. 48, # 11 p. 2883 - 2888
参考文献
LABORATORIOS ALMIRALL, S.A.
Patent: WO2008/77639 A1, 2008 ;
Location in patent: Page/Page column 23 ;
反应条件
in 1-methyl-pyrrolidin-2-one Rosenmund-van Braun Cyanation; 1.5 h; Reflux;
参考文献
Negoro, Kenji; Yonetoku, Yasuhiro; Misawa-Mukai, Hana; Hamaguchi, Wataru; Maruyama, Tatsuya; Yoshida, Shigeru; Takeuchi, Makoto; Ohta, Mitsuaki
Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 17 p. 5235 - 5246
参考文献
Seiko Epson Corporation
Patent: US5354502 A1, 1994 ;
反应条件
sulfuric acid; sodium hydrogencarbonate; copper(II) sulfate; sodium nitrite in cyclohexane; water; acetic acid 1.) -5 deg C, 2.5 h; 2.) 50 deg C;
参考文献
Molecular Crystals and Liquid Crystals (1969-1991), , vol. 172, p. 165 - 190
反应条件
sodium perborate; acetic acid T=65 - 70°C; 21 h; Inert atmosphere;
参考文献
Rueeger, Heinrich; Lueoend, Rainer; Rogel, Olivier; Rondeau, Jean-Michel; Moebitz, Henrik; MacHauer, Rainer; Jacobson, Laura; Staufenbiel, Matthias; Desrayaud, Sandrine; Neumann, Ulf
Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3364 - 3386
反应条件
1.1: 1-methyl-pyrrolidin-2-one / 1.5 h / |Reflux 2.1: sodium nitrite; sulfuric acid; acetic acid / 1 h / 20 °C 2.2: 13.5 h / 20 °C View Scheme
参考文献
Negoro, Kenji; Yonetoku, Yasuhiro; Misawa-Mukai, Hana; Hamaguchi, Wataru; Maruyama, Tatsuya; Yoshida, Shigeru; Takeuchi, Makoto; Ohta, Mitsuaki
Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 17 p. 5235 - 5246