5-氟吲哚-2-甲酸乙酯合成路线 (共 26 条)
反应条件
1: 5-fluoro-1H-indole-2-carboxylic acid ethyl ester With sodium hydride in N,N-dimethyl-formamide
T=0 - 20°C; 1 h;
2: 4-(bromomethyl)pyridine hydrobromide in N,N-dimethyl-formamide
T=0 - 20°C; 21.5 h;
参考文献
SANOFI-AVENTIS
Patent: US2008/146646 A1, 2008 ;
Location in patent: Page/Page column 7; 8 ;
反应条件
tributylphosphine; 1,1'-azodicarbonyl-dipiperidine in toluene
T=20°C; 48 h;
参考文献
SANOFI-AVENTIS
Patent: US2009/42873 A1, 2009 ;
Location in patent: Page/Page column 19 ;
US 20090042873 A1
反应条件
1: 5-fluoro-1H-indole-2-carboxylic acid ethyl ester With sodium hydride in N,N-dimethyl-formamide
T=0 - 20°C; 1 h;
2: 3-(bromomethyl)pyridine hydrobromide in N,N-dimethyl-formamide
T=0 - 20°C; 59.5 h;
参考文献
SANOFI-AVENTIS
Patent: US2008/146646 A1, 2008 ;
Location in patent: Page/Page column 8 ;
反应条件
tributylphosphine; 1,1'-azodicarbonyl-dipiperidine in tetrahydrofuran
T=20°C;
参考文献
SANOFI-AVENTIS
Patent: US2008/146646 A1, 2008 ;
Location in patent: Page/Page column 9 ;
反应条件
1.1: sodium hydroxide / ethanol / 3 h / Reflux
1.2: pH 5 / Cooling with ice
2.1: quinoline; copper / 3 h / Neat (no solvent); Reflux
3.1: acetic acid / 20 h / Reflux
View Scheme
参考文献
Zhang, Fan; Zhao, Yanfang; Sun, Li; Ding, Lu; Gu, Yucheng; Gong, Ping
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 3149 - 3157
反应条件
iodine; potassium hydroxide in N,N-dimethyl-formamide
T=20°C; 1.5 h;
参考文献
Neagoie, Cleopatra; Vedrenne, Emeline; Buron, Frederic; Merour, Jean-Yves; Rosca, Sorin; Bourg, Stephane; Lozach, Olivier; Meijer, Laurent; Baldeyrou, Brigitte; Lansiaux, Amelie; Routier, Sylvain
European Journal of Medicinal Chemistry, 2012 , vol. 49, p. 379 - 396