弗斯特罗定合成路线

弗斯特罗定合成路线（共 67 条）

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反应条件

1: N,N-dimethyl-formamide / 12 h / 80 - 85 °C / Inert atmosphere 2: water; lithium hydroxide hydrate / methanol / 4 h / 25 - 35 °C 3: sodium hydrogencarbonate / dichloromethane; water / 0.5 h / 0 - 5 °C / Inert atmosphere View Scheme

参考文献

WO2012/98560 A2, ;
WO 2012/098560 A2

1390644-47-9

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286930-02-7弗斯特罗定

反应条件

1: water; lithium hydroxide hydrate / methanol / 4 h / 25 - 35 °C 2: sodium hydrogencarbonate / dichloromethane; water / 0.5 h / 0 - 5 °C / Inert atmosphere View Scheme

参考文献

WO2012/98560 A2, ;
WO 2012/098560 A2

754159-68-73-[(1R)-3-[双(1-甲基乙基)氨基]-1-苯基丙基]-4-(苯基甲氧基)苯甲酸

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286930-02-7弗斯特罗定

反应条件

1: sulfuric acid / 20 °C / Reflux 2: sodium bis(2-methoxyethoxy)aluminium dihydride / toluene / 3 h / Inert atmosphere 3: hydrogen / Raney nickel / methanol / 20 °C 4: triethylamine / acetonitrile / -10 °C View Scheme

参考文献

WO2011/145019 A1, ;

1350477-43-8

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286930-02-7弗斯特罗定

反应条件

1: ammonia / water / pH 8 - 9 2: sulfuric acid / 20 °C / Reflux 3: sodium bis(2-methoxyethoxy)aluminium dihydride / toluene / 3 h / Inert atmosphere 4: hydrogen / Raney nickel / methanol / 20 °C 5: triethylamine / acetonitrile / -10 °C View Scheme

参考文献

WO2011/145019 A1, ;

760147-33-9

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286930-02-7弗斯特罗定

反应条件

1: potassium hydroxide / dimethyl sulfoxide / 5.5 h / 110 - 120 °C 2: methanol / 50 - 65 °C 3: ammonia / water / pH 8 - 9 4: sulfuric acid / 20 °C / Reflux 5: sodium bis(2-methoxyethoxy)aluminium dihydride / toluene / 3 h / Inert atmosphere 6: hydrogen / Raney nickel / methanol / 20 °C 7: triethylamine / acetonitrile / -10 °C View Scheme

参考文献

WO2011/145019 A1, ;

140-10-3肉桂酸

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286930-02-7弗斯特罗定

反应条件

1.1: sulfuric acid / 120 - 125 °C 2.1: potassium carbonate; sodium iodide / acetone / Reflux 3.1: sodium tetrahydroborate / ethylene glycol dimethyl ether / 0.17 h 3.2: 3 h / 10 °C 4.1: triethylamine / dichloromethane / 12 h / 25 - 30 °C 5.1: acetonitrile / 30 h / 95 - 100 °C / autoclave; Sealed tube 6.1: isopropyl alcohol / 15 h / 25 - 86 °C 7.1: sodium hydroxide / water 8.1: ethyl bromide; iodine; magnesium / tetrahydrofuran / 1 h / 55 °C / Reflux 8.2: 1 h / -65 - -60 °C 9.1: thionyl chloride / 10 °C / Reflux 10.1: lithium aluminium tetrahydride / tetrahydrofuran / 14 h / 25 - 30 °C 11.1: hydrogen / 5 Pd(II)/C(eggshell) / methanol / 50 - 55 °C 12.1: dichloromethane / 1.5 h / 0 - 5 °C 12.2: 1 h / 0 - 5 °C View Scheme

参考文献

US2011/124903 A1, ;

250214-39-2

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286930-02-7弗斯特罗定

反应条件

1: raney nickel / methanol / 30 - 35 °C / Autoclave 2: tetrahydrofuran / 10 - 55 °C 3: potassium carbonate / toluene; water / 50 - 55 °C 4: dichloromethane / -25 - -20 °C View Scheme

参考文献

WO2011/141932 A2, ;

1349883-68-6

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286930-02-7弗斯特罗定

反应条件

1.1: potassium carbonate / acetone / 20 - 25 °C / Industry scale 1.2: 50 - 60 °C 2.1: pyridine / dichloromethane / 5 - 30 °C / Industry scale 3.1: water / 75 - 78 °C / Industry scale 4.1: ethyl bromide; iodine; magnesium / tetrahydrofuran / 50 - 60 °C 4.2: -70 - -60 °C 4.3: -50 °C 5.1: BH3*S(CH3)2 / tetrahydrofuran / 25 - 50 °C 5.2: 0.5 h / 10 - 15 °C / Industry scale 6.1: raney nickel / methanol / 30 - 35 °C / Autoclave 7.1: tetrahydrofuran / 10 - 55 °C 8.1: potassium carbonate / toluene; water / 50 - 55 °C 9.1: dichloromethane / -25 - -20 °C View Scheme

参考文献

WO2011/141932 A2, ;

1135493-18-3

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286930-02-7弗斯特罗定

反应条件

1.1: sodium hydroxide / water 2.1: ethyl bromide; iodine; magnesium / tetrahydrofuran / 1 h / 55 °C / Reflux 2.2: 1 h / -65 - -60 °C 3.1: thionyl chloride / 10 °C / Reflux 4.1: lithium aluminium tetrahydride / tetrahydrofuran / 14 h / 25 - 30 °C 5.1: hydrogen / 5 Pd(II)/C(eggshell) / methanol / 50 - 55 °C 6.1: dichloromethane / 1.5 h / 0 - 5 °C 6.2: 1 h / 0 - 5 °C View Scheme

参考文献

US2011/124903 A1, ;

108-18-9

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286930-02-7弗斯特罗定

反应条件

1.1: potassium carbonate; potassium iodide / toluene; methanol / 20 h / Reflux 2.1: methanesulfonic acid / 3 h / 100 °C 3.1: sodium tetrahydroborate / methanol / 2 h / 0 °C 3.2: 0.08 h 3.3: pH 8 4.1: 1,1-dimethylpropan-1-ol / 25 - 70 °C 5.1: potassium carbonate / toluene; water / 1 h / 50 °C 6.1: triethylamine / dichloromethane / 0 - 25 °C View Scheme

参考文献

EP2364966 A1, ;

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