6-(4-氟苯基)甲酸吡啶合成路线 （共 5 条）
反应条件
tetrakis(triphenylphosphine) palladium(0); palladium diacetate; sodium carbonate in ethylene glycol dimethyl ether; ethanol; water
T=100°C; 7 h; Inert atmosphere;
参考文献
Bristol-Myers Squibb Company
Patent: US2007/60613 A1, 2007 ;
Location in patent: Page/Page column 18-19 ;
US 20070060613 A1
反应条件
1: 2-bromo-6-pyridine-carboxylic acid With sodium carbonate in ethylene glycol dimethyl ether; water
2: 2-(4-fluorophenyl)-5,5-dimethyl-1,3,2-dioxaborinane With tetrakis(triphenylphosphine) palladium(0) in ethylene glycol dimethyl ether; ethanol; water
T=100°C; 7 h;
3: With trifluoroacetic acid in ethylene glycol dimethyl ether; ethanol; water
参考文献
Borzilleri, Robert M.; Cornelius, Lyndon A.M.; Schmidt, Robert J.; Schroeder, Gretchen M.; Kim, Kyoung S.
Patent: US2005/245530 A1, 2005 ;
Location in patent: Page/Page column 65 ;
US 20050245530 A1
反应条件
lithium hydroxide hydrate; water in methanol
T=80°C; 3 h;
参考文献
CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; ALVAREZ ESCOBAR, Rosa Maria; GARCIA GARCIA, Ana Belen; RIESCO FAGUNDO, Rosario Concepcion; BLANCO APARICIO, Carmen
Patent: WO2012/98387 A1, 2012 ;
Location in patent: Page/Page column 84 ;
WO 2012/098387 A1
反应条件
1: sodium carbonate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / ethylene glycol dimethyl ether / 1.33 h / 75 °C / Inert atmosphere; Microwave irradiation
2: water; lithium hydroxide hydrate / methanol / 3 h / 80 °C
View Scheme
参考文献
CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; ALVAREZ ESCOBAR, Rosa Maria; GARCIA GARCIA, Ana Belen; RIESCO FAGUNDO, Rosario Concepcion; BLANCO APARICIO, Carmen
Patent: WO2012/98387 A1, 2012 ;
WO 2012/098387 A1
反应条件
1: sodium carbonate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / ethylene glycol dimethyl ether / 1.33 h / 75 °C / Inert atmosphere; Microwave irradiation
2: water; lithium hydroxide hydrate / methanol / 3 h / 80 °C
View Scheme
参考文献
CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; ALVAREZ ESCOBAR, Rosa Maria; GARCIA GARCIA, Ana Belen; RIESCO FAGUNDO, Rosario Concepcion; BLANCO APARICIO, Carmen
Patent: WO2012/98387 A1, 2012 ;
WO 2012/098387 A1
