(3R,4S)-1-(4-氟苯基)-3-[(3S)-3-(4-氟苯基)-3-羟基丙基]-4-[4-(苯甲氧基)苯基]-2-氮杂环丁酮合成路线 (共 37 条)
反应条件
1.1: potassium carbonate; potassium iodide / tetrahydrofuran / 20 h / |Reflux 2.1: methanesulfonic acid / acetone / 2 h / 20 °C 3.1: toluene / 72 h / |Reflux 4.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 5.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 5.2: 0.25 h / 20 °C 6.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 7.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 8.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: potassium carbonate; potassium iodide / tetrahydrofuran / 20 h / |Reflux 2.1: methanesulfonic acid / acetone / 2 h / 20 °C 3.1: toluene / 72 h / |Reflux 4.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 5.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 5.2: 0.25 h / 20 °C 6.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 7.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 8.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: methanesulfonic acid / acetone / 2 h / 20 °C 2.1: toluene / 72 h / |Reflux 3.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 4.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 4.2: 0.25 h / 20 °C 5.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 6.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 7.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: pyridine; acetic anhydride / dichloromethane / 2 h / 20 °C 2.1: toluene / 72 h / |Reflux 3.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 4.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 4.2: 0.25 h / 20 °C 5.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 6.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 7.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: zinc; ammonium chloride / water / 0.25 h / 60 °C 2.1: methanesulfonic acid / acetone / 2 h / 20 °C 3.1: toluene / 72 h / |Reflux 4.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 5.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 5.2: 0.25 h / 20 °C 6.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 7.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 8.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: methanesulfonic acid / acetone / 2 h / 20 °C 2.1: toluene / 72 h / |Reflux 3.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 4.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 4.2: 0.25 h / 20 °C 5.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 6.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 7.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: toluene / 72 h / |Reflux 2.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 3.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 3.2: 0.25 h / 20 °C 4.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 5.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 6.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: toluene / 72 h / |Reflux 2.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 3.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 3.2: 0.25 h / 20 °C 4.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 5.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 6.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1.1: potassium iodide; chloro-trimethyl-silane / acetonitrile / 0.58 h / 20 °C 2.1: chloro-trimethyl-silane; 1H-imidazole / dichloromethane / 0.5 h / 20 °C 2.2: 0.25 h / 20 °C 3.1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 4.1: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 5.1: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057
反应条件
1: lithium hydroxide hydrate / tetrahydrofuran; water / 18 h 2: triphenylphosphine; di-isopropyl azodicarboxylate / 3 h / 0 °C 3: 1,1-dimethylethylmagnesium chloride / diethyl ether / 2 h / 0 °C View Scheme
参考文献
Journal of Organic Chemistry, , vol. 78, # 14 p. 7048 - 7057