2-(4-(乙氧基羰基)苯基)乙酸合成路线 （共 8 条）
反应条件
1: With lithium hydroxide hydrate in tetrahydrofuran; ethanol; water
T=20°C;
2: With hydrogenchloride in water
pH=3;
参考文献
N30 PHARMACEUTICALS, LLC; SUN, Xicheng; QIU, Jian; WASLEY, Jan
Patent: WO2011/99978 A1, 2011 ;
Location in patent: Page/Page column 37-38 ;
WO 2011/099978 A1
反应条件
sodium hydroxide; water
T=20°C; 0.666667 h;
参考文献
Kissei Pharmaceutical Co., Ltd.
Patent: EP1443041 A1, 2004 ;
Location in patent: Page 19 ;
反应条件
1.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 2 h / 20 °C
2.1: dichloromethane / 2 h / 20 °C
3.1: lithium hydroxide hydrate / ethanol; water; tetrahydrofuran / 20 °C
3.2: pH 3
View Scheme
参考文献
N30 PHARMACEUTICALS, LLC; SUN, Xicheng; QIU, Jian; WASLEY, Jan
Patent: WO2011/99978 A1, 2011 ;
WO 2011/099978 A1
反应条件
1.1: carbon disulfide; AlCl3, aluminium chloride / 0.17 h / 0 - 10 °C
1.2: 0 - 10 °C / Reflux
2.1: sodium hydroxide; lithium hydroxide hydrate / tetrahydrofuran / 20 °C
2.2: 2.5 h / 20 - 90 °C
3.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 2 h / 20 °C
4.1: dichloromethane / 2 h / 20 °C
5.1: lithium hydroxide hydrate / ethanol; water; tetrahydrofuran / 20 °C
5.2: pH 3
View Scheme
参考文献
N30 PHARMACEUTICALS, LLC; SUN, Xicheng; QIU, Jian; WASLEY, Jan
Patent: WO2011/99978 A1, 2011 ;
WO 2011/099978 A1
反应条件
1.1: sodium hydroxide; lithium hydroxide hydrate / tetrahydrofuran / 20 °C
1.2: 2.5 h / 20 - 90 °C
2.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 2 h / 20 °C
3.1: dichloromethane / 2 h / 20 °C
4.1: lithium hydroxide hydrate / ethanol; water; tetrahydrofuran / 20 °C
4.2: pH 3
View Scheme
参考文献
N30 PHARMACEUTICALS, LLC; SUN, Xicheng; QIU, Jian; WASLEY, Jan
Patent: WO2011/99978 A1, 2011 ;
WO 2011/099978 A1
反应条件
1: aq. HCl / 1.5 h / 20 - 23 °C
2: aq. NaNO2, HCl / 2 h / 35 °C
View Scheme
参考文献
Grell, Wolfgang; Hurnaus, Rudolf
Journal of Medicinal Chemistry, 1998 , vol. 41, # 26 p. 5219 - 5246
反应条件
1.1: dichloromethane / 2 h / 20 °C
2.1: lithium hydroxide hydrate / ethanol; water; tetrahydrofuran / 20 °C
2.2: pH 3
View Scheme
参考文献
N30 PHARMACEUTICALS, LLC; SUN, Xicheng; QIU, Jian; WASLEY, Jan
Patent: WO2011/99978 A1, 2011 ;
WO 2011/099978 A1
反应条件
sodium azide; [bis(acetoxy)iodo]benzene in acetonitrile
T=0 - 20°C; 0.416667 h;
参考文献
Telvekar, Vikas N.; Sasane, Kulbhushan A.
Synlett, 2010 , # 18 p. 2778 - 2780
