5-溴-2-甲基-1H-吡咯并[2,3-b]吡啶合成路线 （共 9 条）
反应条件
potassium tert-butylate in tert-butyl alcohol T=85°C; 1 h;
参考文献
F. HOFFMANN-LA ROCHE AG; DYKE, Hazel Joan; GAZZARD, Lewis J.; WILLIAMS, Karen
Patent: WO2011/73263 A1, 2011 ;
Location in patent: Page/Page column 79 ;
WO 2011/073263 A1
反应条件
sodium hydroxide in methanol 2 h; Reflux;
参考文献
UNIVERSITY OF ROCHESTER; BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA; GELBARD, Harris A.; DEWHURST, Stephen; GENDELMAN, Howard E.
Patent: WO2014/85795 A1, 2014 ;
Location in patent: Paragraph 0394 ;
反应条件
1: triethylamine / copper(l) iodide; bis-triphenylphosphine-palladium(II) chloride / tetrahydrofuran / 1 h / 0 - 20 °C 2: potassium tert-butylate / tert-butyl alcohol / 1 h / 85 °C View Scheme
参考文献
WO2011/73263 A1, ;
WO 2011/073263 A1
反应条件
1.1: sulfuric acid; KIO3 / 100 °C 1.2: 1.5 h 2.1: triethylamine / copper(l) iodide; bis-triphenylphosphine-palladium(II) chloride / tetrahydrofuran / 1 h / 0 - 20 °C 3.1: potassium tert-butylate / tert-butyl alcohol / 1 h / 85 °C View Scheme
参考文献
WO2011/73263 A1, ;
WO 2011/073263 A1
反应条件
1.1: sodium hydroxide; tetrabutylammomium bromide / dichloromethane / 2 h / 0 °C 2.1: diisopropylamine; n-butyllithium / hexane; tetrahydrofuran / 0.5 h / -35 °C 2.2: 2 h / -35 - 20 °C 3.1: sodium hydroxide / methanol / 2 h / Reflux View Scheme
参考文献
WO2011/149950 A2, ;
WO 2011/149950 A2
反应条件
1.1: diisopropylamine; n-butyllithium / hexane; tetrahydrofuran / 0.5 h / -35 °C 1.2: 2 h / -35 - 20 °C 2.1: sodium hydroxide / methanol / 2 h / Reflux View Scheme
参考文献
WO2011/149950 A2, ;
WO 2011/149950 A2
反应条件
1: 5-bromo-2-methyl-1H-pyrrolo[2,3-b]pyridine With AlCl3, aluminium chloride in dichloromethane 0.833333 h; 2: 2,2,2-trichloroacetyl chloride in dichloromethane 18 h; 3: methanol
参考文献
F. HOFFMANN-LA ROCHE AG; DYKE, Hazel Joan; GAZZARD, Lewis J.; WILLIAMS, Karen
Patent: WO2011/73263 A1, 2011 ;
Location in patent: Page/Page column 79-80 ;
WO 2011/073263 A1
反应条件
1.1: AlCl3, aluminium chloride / dichloromethane / 0.83 h 1.2: 18 h 2.1: sodium hydroxide; N-benzyl-N,N,N-triethylammonium chloride / dichloromethane / 1.33 h / 0 - 20 °C 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
potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in N,N-dimethyl-formamide
T=80°C;
参考文献
PFIZER INC.
Patent: WO2009/16460 A2, 2009 ;
Location in patent: Page/Page column 74-75 ;
WO 2009/016460 A2
