4-(5-溴-2-氯苄基)苯酚合成路线 （共 8 条）
反应条件
1.1: triethylamine / acetonitrile / 2 h / 5 - 15 °C 2.1: n-butyllithium / tetrahydrofuran; hexane; toluene / 0.5 h / -65 °C / |Inert atmosphere 2.2: 3 h / -65 - -55 °C 2.3: 16 h / 20 - 25 °C 3.1: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / 2 h / -30 - -10 °C / |Inert atmosphere 4.1: caesium carbonate; tetra-(n-butyl)ammonium iodide / N,N-dimethyl-formamide / 12 h / 40 °C / |Inert atmosphere View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 57, # 4 p. 1236 - 1251
反应条件
1: With boron trichloride in dichloromethane
T=0°C; 0.5 h; Inert atmosphere;
2: With boron tribromide in dichloromethane
T=0°C;
参考文献
PFIZER INC.; MASCITTI, Vincent
Patent: WO2011/51864 A1, 2011 ;
Location in patent: Page/Page column 27-28 ;
WO 2011/051864 A1
反应条件
triethylsilane; boron trifluoride diethyl etherate in diethyl ether; dichloromethane; acetonitrile
T=20°C; 16 h; Inert atmosphere;
参考文献
HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; MANOHAR SHARMA, Vedula; RATHNAKAR REDDY, Kura; VL SUBRAHMANYAM, Lanka; SUDHAKAR, Neela
Patent: WO2012/25857 A1, 2012 ;
Location in patent: Page/Page column 21 ;
WO 2012/025857 A1
反应条件
1: thionyl chloride / dichloromethane; N,N-dimethyl-formamide / 12 h / 20 °C
2: AlCl3, aluminium chloride / dichloromethane / 1 h / 0 °C
3: AlCl3, aluminium chloride / dichloromethane / 12 h / 20 °C / Inert atmosphere
4: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; diethyl ether; acetonitrile / 16 h / 20 °C / Inert atmosphere
View Scheme
参考文献
HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; MANOHAR SHARMA, Vedula; RATHNAKAR REDDY, Kura; VL SUBRAHMANYAM, Lanka; SUDHAKAR, Neela
Patent: WO2012/25857 A1, 2012 ;
WO 2012/025857 A1
反应条件
1: AlCl3, aluminium chloride / dichloromethane / 1 h / 0 °C
2: AlCl3, aluminium chloride / dichloromethane / 12 h / 20 °C / Inert atmosphere
3: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; diethyl ether; acetonitrile / 16 h / 20 °C / Inert atmosphere
View Scheme
参考文献
HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; MANOHAR SHARMA, Vedula; RATHNAKAR REDDY, Kura; VL SUBRAHMANYAM, Lanka; SUDHAKAR, Neela
Patent: WO2012/25857 A1, 2012 ;
WO 2012/025857 A1
反应条件
1: AlCl3, aluminium chloride / dichloromethane / 12 h / 20 °C / Inert atmosphere
2: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; diethyl ether; acetonitrile / 16 h / 20 °C / Inert atmosphere
View Scheme
参考文献
HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; MANOHAR SHARMA, Vedula; RATHNAKAR REDDY, Kura; VL SUBRAHMANYAM, Lanka; SUDHAKAR, Neela
Patent: WO2012/25857 A1, 2012 ;
WO 2012/025857 A1
反应条件
1.1: potassium carbonate / acetone / 0.5 h / 20 °C
1.2: 3 h / Reflux
2.1: AlCl3, aluminium chloride / dichloromethane / 1 h / 0 °C
3.1: AlCl3, aluminium chloride / dichloromethane / 12 h / 20 °C / Inert atmosphere
4.1: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; diethyl ether; acetonitrile / 16 h / 20 °C / Inert atmosphere
View Scheme
参考文献
HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; MANOHAR SHARMA, Vedula; RATHNAKAR REDDY, Kura; VL SUBRAHMANYAM, Lanka; SUDHAKAR, Neela
Patent: WO2012/25857 A1, 2012 ;
WO 2012/025857 A1
反应条件
1: AlCl3, aluminium chloride / dichloromethane / 1 h / 0 °C
2: AlCl3, aluminium chloride / dichloromethane / 12 h / 20 °C / Inert atmosphere
3: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; diethyl ether; acetonitrile / 16 h / 20 °C / Inert atmosphere
View Scheme
参考文献
HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; MANOHAR SHARMA, Vedula; RATHNAKAR REDDY, Kura; VL SUBRAHMANYAM, Lanka; SUDHAKAR, Neela
Patent: WO2012/25857 A1, 2012 ;
WO 2012/025857 A1
