8-氟-2-甲基-2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚合成路线 （共 6 条）
反应条件
1: 1-(4-fluorophenyl)-hydrazine hydrochloride With sulfuric acid in 1,4-dioxane
T=20°C; 0.0833333 h;
2: N-methyl-4-piperidone in 1,4-dioxane
T=80°C; 2 h;
3: With potassium hydroxide in water
pH=10; Product distribution / selectivity;
参考文献
MEDIVATION TECHNOLOGIES, INC.; HUNG, David, T.; PROTTER, Andrew, Asher; JAIN, Rajendra, Parasmal; CHAKRAVARTY, Sarvajit; GIORGETTI, Marco
Patent: WO2010/51501 A1, 2010 ;
Location in patent: Page/Page column 243-244 ;
反应条件
sodium tetrahydroborate in methanol; water
T=20 - 100°C; Inert atmosphere;
参考文献
Dong, Huijun; Latka, Regina T.; Driver, Tom G.
Organic Letters, 2011 , vol. 13, # 10 p. 2726 - 2729
反应条件
1: dichloromethane / 20 °C / Inert atmosphere
2: ruthenium(III) chloride polyhydrate / isopropanol acetate / 15 h / 80 °C / Inert atmosphere
3: sodium tetrahydroborate / methanol; water / 20 - 100 °C / Inert atmosphere
View Scheme
参考文献
Dong, Huijun; Latka, Regina T.; Driver, Tom G.
Organic Letters, 2011 , vol. 13, # 10 p. 2726 - 2729
反应条件
1: ruthenium(III) chloride polyhydrate / isopropanol acetate / 15 h / 80 °C / Inert atmosphere
2: sodium tetrahydroborate / methanol; water / 20 - 100 °C / Inert atmosphere
View Scheme
参考文献
Dong, Huijun; Latka, Regina T.; Driver, Tom G.
Organic Letters, 2011 , vol. 13, # 10 p. 2726 - 2729
反应条件
1.1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium carbonate / 1,4-dioxane; water / 2.5 h / 80 °C / Inert atmosphere
2.1: acetic acid; sodium nitrite / water / 1.5 h / 0 °C / Inert atmosphere
2.2: 0 - 20 °C / Inert atmosphere
3.1: dichloromethane / 20 °C / Inert atmosphere
4.1: ruthenium(III) chloride polyhydrate / isopropanol acetate / 15 h / 80 °C / Inert atmosphere
5.1: sodium tetrahydroborate / methanol; water / 20 - 100 °C / Inert atmosphere
View Scheme
参考文献
Dong, Huijun; Latka, Regina T.; Driver, Tom G.
Organic Letters, 2011 , vol. 13, # 10 p. 2726 - 2729
反应条件
1.1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium carbonate / 1,4-dioxane; water / 2.5 h / 80 °C / Inert atmosphere
2.1: acetic acid; sodium nitrite / water / 1.5 h / 0 °C / Inert atmosphere
2.2: 0 - 20 °C / Inert atmosphere
3.1: dichloromethane / 20 °C / Inert atmosphere
4.1: ruthenium(III) chloride polyhydrate / isopropanol acetate / 15 h / 80 °C / Inert atmosphere
5.1: sodium tetrahydroborate / methanol; water / 20 - 100 °C / Inert atmosphere
View Scheme
参考文献
Dong, Huijun; Latka, Regina T.; Driver, Tom G.
Organic Letters, 2011 , vol. 13, # 10 p. 2726 - 2729
