2-氨基-5-氟-3-吲哚吡啶合成路线 (共 6 条)
反应条件
1: With sulfuric acid in water 1.5 h; Heating / reflux; 2: With sodium hydroxide in dichloromethane; water pH=12;
参考文献
F. HOFFMANN-LA ROCHE AG; VERNALIS RESEARCH LIMITED
Patent: WO2005/849 A1, 2005 ;
Location in patent: Page/Page column 112 ;
反应条件
sodium periodate; sulfuric acid; sodium iodide in water T=100°C; 1 h; Heating / reflux;
参考文献
AVEXA LIMITED
Patent: WO2008/77188 A1, 2008 ;
Location in patent: Page/Page column 136 ;
反应条件
1: With N-iodo-succinimide in acetic acid T=70°C; 6 h; 2: With sodium hydrogencarbonate in water pH=~ 8;
参考文献
US2008/45561 A1, ;
Page/Page column 30 ;
反应条件
1,4-diaza-bicyclo[2.2.2]octane; palladium diacetate in N,N-dimethyl-formamide T=100°C; 2.83333 h;
参考文献
SANOFI-AVENTIS
Patent: US2009/298865 A1, 2009 ;
Location in patent: Page/Page column 5 ;
US 20090298865 A1
反应条件
1.1: triethylamine / copper(l) iodide; bis-triphenylphosphine-palladium(II) chloride / tetrahydrofuran / 1 h / 0 - 20 °C 2.1: potassium tert-butylate / tert-butyl alcohol / 1 h / 85 °C 3.1: AlCl3, aluminium chloride / dichloromethane / 0.83 h 3.2: 18 h View Scheme
参考文献
F. HOFFMANN-LA ROCHE AG; DYKE, Hazel Joan; GAZZARD, Lewis J.; WILLIAMS, Karen
Patent: WO2011/73263 A1, 2011 ;
WO 2011/073263 A1
反应条件
copper(l) iodide; triethylamine; bis-triphenylphosphine-palladium(II) chloride in N,N-dimethyl-formamide
T=50°C; 8 h;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2008/4117 A1, 2008 ;
Location in patent: Page/Page column 105 ;