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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
盐酸伊立替康
合成路线
(共 17 条)
456-48-4
3-氟苯甲醛
→
反应条件
100286-90-6
盐酸伊立替康
反应条件
1.1: hydroxylamine hydrochloride; sodium hydroxide; water / ethanol / 4 h / 5 °C 2.1: acetic anhydride / 2 h / 110 °C 3.1: magnesium / tetrahydrofuran / 0.5 h / 40 °C 3.2: 1 h / 40 °C 4.1: nitric acid / dichloromethane / 12 h / 10 - 20 °C 5.1: sodium hydroxide / 2 h / 0 - 20 °C 6.1: lithium chloride / N,N-dimethyl-formamide / 6 h / |Reflux 7.1: sodium carbonate; sodium dithionite; water / 1 h / 20 °C 8.1: trifluoroacetic acid / toluene / 6 h / 80 °C 9.1: triethylamine; pyridine / 2 h / 20 °C / |Inert atmosphere 10.1: hydrogenchloride; water / 3 h / 20 - 70 °C View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
458-02-6
3-氟苯甲醛肟
→
反应条件
100286-90-6
盐酸伊立替康
反应条件
1.1: acetic anhydride / 2 h / 110 °C 2.1: magnesium / tetrahydrofuran / 0.5 h / 40 °C 2.2: 1 h / 40 °C 3.1: nitric acid / dichloromethane / 12 h / 10 - 20 °C 4.1: sodium hydroxide / 2 h / 0 - 20 °C 5.1: lithium chloride / N,N-dimethyl-formamide / 6 h / |Reflux 6.1: sodium carbonate; sodium dithionite; water / 1 h / 20 °C 7.1: trifluoroacetic acid / toluene / 6 h / 80 °C 8.1: triethylamine; pyridine / 2 h / 20 °C / |Inert atmosphere 9.1: hydrogenchloride; water / 3 h / 20 - 70 °C View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
403-54-3
3-氟苯腈
→
反应条件
100286-90-6
盐酸伊立替康
反应条件
1.1: magnesium / tetrahydrofuran / 0.5 h / 40 °C 1.2: 1 h / 40 °C 2.1: nitric acid / dichloromethane / 12 h / 10 - 20 °C 3.1: sodium hydroxide / 2 h / 0 - 20 °C 4.1: lithium chloride / N,N-dimethyl-formamide / 6 h / |Reflux 5.1: sodium carbonate; sodium dithionite; water / 1 h / 20 °C 6.1: trifluoroacetic acid / toluene / 6 h / 80 °C 7.1: triethylamine; pyridine / 2 h / 20 °C / |Inert atmosphere 8.1: hydrogenchloride; water / 3 h / 20 - 70 °C View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
455-67-4
3-氟苯丙酮
→
反应条件
100286-90-6
盐酸伊立替康
反应条件
1: nitric acid / dichloromethane / 12 h / 10 - 20 °C 2: sodium hydroxide / 2 h / 0 - 20 °C 3: lithium chloride / N,N-dimethyl-formamide / 6 h / |Reflux 4: sodium carbonate; sodium dithionite; water / 1 h / 20 °C 5: trifluoroacetic acid / toluene / 6 h / 80 °C 6: triethylamine; pyridine / 2 h / 20 °C / |Inert atmosphere 7: hydrogenchloride; water / 3 h / 20 - 70 °C View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
100286-90-6
盐酸伊立替康
→
反应条件
86639-52-3
7-乙基-10-羟基喜树碱
反应条件
di-p-nitrophenylphosphoric acid in aq. buffer T=37°C; pH=7.5; Enzymatic reaction; Reagent/catalyst;
参考文献
Ishizuka, Tomoko; Yoshigae, Yasushi; Murayama, Nobuyuki; Izumi, Takashi
Drug Metabolism and Disposition, 2013 , vol. 41, # 11 p. 1888 - 1895
100286-90-6
盐酸伊立替康
→
反应条件
86639-52-3
7-乙基-10-羟基喜树碱
反应条件
di-p-nitrophenylphosphoric acid in aq. buffer T=37°C; pH=7.5; Enzymatic reaction; Reagent/catalyst;
参考文献
Ishizuka, Tomoko; Yoshigae, Yasushi; Murayama, Nobuyuki; Izumi, Takashi
Drug Metabolism and Disposition, 2013 , vol. 41, # 11 p. 1888 - 1895
100286-90-6
盐酸伊立替康
→
反应条件
136572-09-3
盐酸伊立替康三水合物
反应条件
hydrogenchloride; water in ethanol T=75 - 80°C;
参考文献
FERMION OY
Patent: WO2006/84941 A2, 2006 ;
Location in patent: Page/Page column 6 ;
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