2-(4-溴苯基)-4,5,6,7-四氢噁唑并[4,5-c]吡啶合成路线 （共 6 条）
反应条件
1: With 1-chloroethyl chlorocarbonate; N-ethyl-N,N-diisopropylamine in 1,2-dichloro-ethane
T=0°C; 2.16667 h; Reflux;
2: With methanol in 1,2-dichloro-ethane
T=20°C; 48 h;
参考文献
ABBOTT HEALTHCARE PRODUCTS B.V.; SMID, Pieter; IWEMA BAKKER, Wouter, I.; COOLEN, Hein, K.A.C.; SLIEDREGT, Leonardus, A.J.M.; VAN DONGEN, Maria, J.P.; DEN HARTOG, Jacobus, A.J.
Patent: WO2012/4373 A1, 2012 ;
Location in patent: Page/Page column 44 ;
WO 2012/004373 A1
反应条件
1.1: triethylamine / dichloromethane / 16 h / 20 °C
2.1: triethylamine; triphenylphosphine; 1,2,2-trichloro-1,1,2-trichloro-ethane / dichloromethane / 64 h / 20 °C
3.1: N,N-dimethyl-formamide / 16 h
4.1: sodium tetrahydroborate / methanol / 18 h / 0 - 20 °C
4.2: 0.08 h
5.1: N-ethyl-N,N-diisopropylamine; 1-chloroethyl chlorocarbonate / 1,2-dichloro-ethane / 2.17 h / 0 °C / Reflux
5.2: 48 h / 20 °C
View Scheme
参考文献
ABBOTT HEALTHCARE PRODUCTS B.V.; SMID, Pieter; IWEMA BAKKER, Wouter, I.; COOLEN, Hein, K.A.C.; SLIEDREGT, Leonardus, A.J.M.; VAN DONGEN, Maria, J.P.; DEN HARTOG, Jacobus, A.J.
Patent: WO2012/4373 A1, 2012 ;
WO 2012/004373 A1
反应条件
1.1: triethylamine / dichloromethane / 16 h / 20 °C
2.1: triethylamine; triphenylphosphine; 1,2,2-trichloro-1,1,2-trichloro-ethane / dichloromethane / 64 h / 20 °C
3.1: N,N-dimethyl-formamide / 16 h
4.1: sodium tetrahydroborate / methanol / 18 h / 0 - 20 °C
4.2: 0.08 h
5.1: N-ethyl-N,N-diisopropylamine; 1-chloroethyl chlorocarbonate / 1,2-dichloro-ethane / 2.17 h / 0 °C / Reflux
5.2: 48 h / 20 °C
View Scheme
参考文献
ABBOTT HEALTHCARE PRODUCTS B.V.; SMID, Pieter; IWEMA BAKKER, Wouter, I.; COOLEN, Hein, K.A.C.; SLIEDREGT, Leonardus, A.J.M.; VAN DONGEN, Maria, J.P.; DEN HARTOG, Jacobus, A.J.
Patent: WO2012/4373 A1, 2012 ;
WO 2012/004373 A1
反应条件
1.1: N,N-dimethyl-formamide / 16 h
2.1: sodium tetrahydroborate / methanol / 18 h / 0 - 20 °C
2.2: 0.08 h
3.1: N-ethyl-N,N-diisopropylamine; 1-chloroethyl chlorocarbonate / 1,2-dichloro-ethane / 2.17 h / 0 °C / Reflux
3.2: 48 h / 20 °C
View Scheme
参考文献
ABBOTT HEALTHCARE PRODUCTS B.V.; SMID, Pieter; IWEMA BAKKER, Wouter, I.; COOLEN, Hein, K.A.C.; SLIEDREGT, Leonardus, A.J.M.; VAN DONGEN, Maria, J.P.; DEN HARTOG, Jacobus, A.J.
Patent: WO2012/4373 A1, 2012 ;
WO 2012/004373 A1
反应条件
1.1: triethylamine; triphenylphosphine; 1,2,2-trichloro-1,1,2-trichloro-ethane / dichloromethane / 64 h / 20 °C
2.1: N,N-dimethyl-formamide / 16 h
3.1: sodium tetrahydroborate / methanol / 18 h / 0 - 20 °C
3.2: 0.08 h
4.1: N-ethyl-N,N-diisopropylamine; 1-chloroethyl chlorocarbonate / 1,2-dichloro-ethane / 2.17 h / 0 °C / Reflux
4.2: 48 h / 20 °C
View Scheme
参考文献
ABBOTT HEALTHCARE PRODUCTS B.V.; SMID, Pieter; IWEMA BAKKER, Wouter, I.; COOLEN, Hein, K.A.C.; SLIEDREGT, Leonardus, A.J.M.; VAN DONGEN, Maria, J.P.; DEN HARTOG, Jacobus, A.J.
Patent: WO2012/4373 A1, 2012 ;
WO 2012/004373 A1
反应条件
1.1: sodium tetrahydroborate / methanol / 18 h / 0 - 20 °C
1.2: 0.08 h
2.1: N-ethyl-N,N-diisopropylamine; 1-chloroethyl chlorocarbonate / 1,2-dichloro-ethane / 2.17 h / 0 °C / Reflux
2.2: 48 h / 20 °C
View Scheme
参考文献
ABBOTT HEALTHCARE PRODUCTS B.V.; SMID, Pieter; IWEMA BAKKER, Wouter, I.; COOLEN, Hein, K.A.C.; SLIEDREGT, Leonardus, A.J.M.; VAN DONGEN, Maria, J.P.; DEN HARTOG, Jacobus, A.J.
Patent: WO2012/4373 A1, 2012 ;
WO 2012/004373 A1
