2-(5-溴-2-氟苯基)-2-氧代乙酸乙酯合成路线 （共 3 条）
反应条件
1: 4-bromo-1-fluoro-2-iodobenzene With isopropylmagnesium chloride in tetrahydrofuran
T=-40 - -30°C;
2: oxalic acid diethyl ester in tetrahydrofuran
T=-70 - -10°C; 1 h;
3: With hydrogenchloride in tetrahydrofuran; water
Cooling;
参考文献
F. HOFFMANN-LA ROCHE AG; SIENA BIOTECH S.P.A; ANDREINI, Matteo; BANNER, David; GUBA, Wolfgang; HILPERT, Hans; MAUSER, Harald; MAYWEG, Alexander, V.; NARQUIZIAN, Robert; POWER, Eoin; ROGERS-EVANS, Mark; TRAVAGLI, Massimiliano; VALACCHI, Michela; WOLTERING, Thomas; WOSTL, Wolfgang
Patent: WO2011/20806 A1, 2011 ;
Location in patent: Page/Page column 84; 85 ;
反应条件
acetic anhydride in dimethyl sulfoxide
T=90°C; 3 h;
参考文献
PHARMACIA and UPJOHN COMPANY
Patent: WO2004/18428 A1, 2004 ;
Location in patent: Page 105-106 ;
反应条件
1: 1-bromo-4-fluorobenzene With n-butyllithium; diisopropylamine in tetrahydrofuran; hexane
T=-70 - -60°C; 2.5 h;
2: oxalic acid diethyl ester in tetrahydrofuran; hexane
T=-70 - -50°C; 0.25 h;
3: With hydrogenchloride; water in tetrahydrofuran; hexane
T=-70°C;
参考文献
NOVARTIS AG; HURTH, Konstanze; LUEOEND, Rainer Martin; MACHAUER, Rainer; NEUMANN, Ulf; RUEEGER, Heinrich; SCHAEFER, Michael; TINTELNOT-BLOMLEY, Marina; VEENSTRA, Siem Jacob; VOEGTLE, Markus
Patent: WO2012/95463 A1, 2012 ;
Location in patent: Page/Page column 67 ;
