1-((1-溴-3-氯丙烷-2-基氧基)甲基)苯合成路线 （共 6 条）
反应条件
2: aq. 4M KOH / H2O; ethanol / 5 h / Heating View Scheme
参考文献
AMGEN INC.; ALLEN, Jennifer; FROHN, Michael; HARRINGTON, Paul; PICKRELL, Alexander; RZASA, Robert; SHAM, Kelvin; HU, Essa
Patent: WO2011/143366 A1, 2011 ;
WO 2011/143366 A1
反应条件
1: diethyl malonate With sodium hydride in 1,4-dioxane; mineral oil T=20°C; 2: 1-Bromo-2-benzyloxy-3-chloro-propane in 1,4-dioxane; mineral oil T=20°C; Reflux; 3: With sodium hydride in 1,4-dioxane; mineral oil Cooling with ice bathReflux;
参考文献
INCYTE CORPORATION
Patent: US2009/233903 A1, 2009 ;
Location in patent: Page/Page column 40-41 ;
US 20090233903 A1
反应条件
1.1: ethanol; sodium / 3 h / Inert atmosphere; Reflux 2.1: potassium hydroxide / ethanol; water / 0.75 h / Inert atmosphere; Reflux 2.2: pH 2 - 3 / Inert atmosphere 3.1: pyridine / 12 h / 120 °C 4.1: N-ethyl-N,N-diisopropylamine; diphenyl phosphoryl azide / toluene / 7 h / 80 °C / Inert atmosphere 4.2: 1 h / 0 - 20 °C / Inert atmosphere View Scheme
参考文献
AMGEN INC.; ALLEN, Jennifer; FROHN, Michael; HARRINGTON, Paul; PICKRELL, Alexander; RZASA, Robert; SHAM, Kelvin; HU, Essa
Patent: WO2011/143366 A1, 2011 ;
WO 2011/143366 A1
反应条件
2: aq. 4M KOH / H2O; ethanol / 5 h / Heating 3: 88.6 percent / 215 °C / 0.4 Torr View Scheme
参考文献
Wiberg,K.B. et al.
Tetrahedron, 1965 , vol. 21, p. 2749 - 2769
参考文献
GLAXO GROUP LIMITED
Patent: WO2007/62332 A2, 2007 ;
Location in patent: Page/Page column 15 ;
反应条件
1: 30 percent / sodium ethoxide / ethanol / 42 h / Heating
2: 92 percent / KOH / aq. ethanol / 1.5 h / Heating
3: 83 percent / 1. 150 deg C, 1 h, 4.0E3 Pa; 2. 165 deg C, 2.5 h; 3. 180 deg C, 2.5 h
4: 81 percent / H2SO4 / CHCl3 / 16 h / Heating
View Scheme
参考文献
Wiberg,K.B. et al.
Tetrahedron, 1965 , vol. 21, p. 2749 - 2769
