2-氟-6-(嘧啶-2-基)苯甲酸甲酯合成路线 （共 5 条）
反应条件
sodium carbonate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct in 2-methyl tetrahydrofuran; water T=74°C; 2.5 h; Inert atmosphere;
参考文献
JANSSEN PHARMACEUTICA NV; LETAVIC, Michael; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHIREMAN, Brock, T.; SWANSON, Devin
Patent: WO2012/145581 A1, 2012 ;
Location in patent: Page/Page column 53-54; 98 ;
WO 2012/145581 A1
反应条件
copper(l) iodide; tetrakis(triphenylphosphine) palladium(0); cesium fluoride in N,N-dimethyl-formamide T=115°C; 0.75 h; Inert atmosphere;
参考文献
ROTTAPHARM SPA; STASI, Luigi Piero; ROVATI, Lucio Claudio; ARTUSI, Roberto; COLACE, Fabrizio; MANDELLI, Stefano; PERUGINI, Lorenzo
Patent: WO2013/92893 A1, 2013 ;
Location in patent: Page/Page column 45 ;
反应条件
1.1: lithium hydroxide hydrate / tetrahydrofuran / 2 h / 50 °C 1.2: 2 h / 65 °C 2.1: isopropylmagnesium chloride / tetrahydrofuran / 0.17 h / 0 °C 2.2: 0.5 h / 0 - 20 °C 3.1: sodium carbonate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / water; 2-methyl tetrahydrofuran / 2.5 h / 74 °C View Scheme
参考文献
JANSSEN PHARMACEUTICA NV; BRANSTETTER, Bryan, James; LETAVIC, Michael, A.; LY, Kiev, S.; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.
Patent: WO2011/50202 A1, 2011 ;
WO 2011/050202 A1
反应条件
1.1: isopropylmagnesium chloride / tetrahydrofuran / 0.17 h / 0 °C 1.2: 0.5 h / 0 - 20 °C 2.1: sodium carbonate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / water; 2-methyl tetrahydrofuran / 2.5 h / 74 °C View Scheme
参考文献
JANSSEN PHARMACEUTICA NV; BRANSTETTER, Bryan, James; LETAVIC, Michael, A.; LY, Kiev, S.; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.
Patent: WO2011/50202 A1, 2011 ;
WO 2011/050202 A1
反应条件
1.1: dichloromethane; N,N-dimethyl-formamide 2.1: isopropylmagnesium chloride / tetrahydrofuran / 0.17 h / 0 °C 2.2: 0.5 h / 20 °C 3.1: water; sodium carbonate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 2-methyl tetrahydrofuran / 2.5 h / 74 °C View Scheme
参考文献
ROTTAPHARM SPA; STASI, Luigi Piero; ROVATI, Lucio Claudio; ARTUSI, Roberto; COLACE, Fabrizio; MANDELLI, Stefano; PERUGINI, Lorenzo
Patent: WO2013/92893 A1, 2013 ;
