7-乙基-10-羟基喜树碱合成路线 （共 84 条）
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 View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
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 View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
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 View Scheme
参考文献
Synthetic Communications, , vol. 43, # 12 p. 1661 - 1667
反应条件
Tris-HCl buffer; human liver carboxylesterase pI 4.5 T=37°C; Hydrolysis; pH=7.4; Enzyme kinetics; Further Variations:Reagents;
参考文献
Biological and Pharmaceutical Bulletin, , vol. 20, # 8 p. 869 - 873
反应条件
4-(N,N-dimethlyamino)pyridine in acetonitrile T=75°C; 5 h; Sonication;
参考文献
PLIVA-LACHEMA A.S.
Patent: WO2005/19223 A1, 2005 ;
Location in patent: Page/Page column 4 ;
反应条件
pyridine; acetamide; triethylamine in dichloromethane T=30 - 40°C; 2 h; Inert atmosphere; Product distribution / selectivity;
参考文献
CADILA HEALTHCARE LIMITED
Patent: EP2341046 A2, 2011 ;
Location in patent: Page/Page column 9 ;
反应条件
1: phosgene; 4-(1-piperidyl)piperidine in dichloromethane T=-10 - 20°C; 3 h; 2: SN-387 lactone in pyridine 0.5 - 2 h;
参考文献
Phytogen Life Sciences Inc.
Patent: US2005/267141 A1, 2005 ;
Location in patent: Page/Page column 6 ;
反应条件
1: bis(trichloromethyl) carbonate; SN-387 lactone With 1,4-diaza-bicyclo[2.2.2]octane; N-ethyl-N,N-diisopropylamine in dichloromethane T=20°C; 0.583333 h; 2: 4-(1-piperidyl)piperidine in dichloromethane T=22 - 25°C; 2.25 - 4.25 h; Product distribution / selectivity;
参考文献
W. C. HERAEUS GMBH
Patent: US2007/135471 A1, 2007 ;
Location in patent: Page/Page column 4 ;
反应条件
1: 3.4 percent / K2CO3 / acetone / 6 h / Heating 2: 59.2 percent / 0.2 N aq. NaOH / acetone / 2 h / Ambient temperature View Scheme
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 40, # 1 p. 131 - 135
反应条件
Tris-HCl buffer; human liver microsomes; magnesium chloride T=37°C; pH=7.4; 0.666667 h; Enzyme kinetics; Further Variations:Reagents;
参考文献
Xenobiotica, , vol. 31, # 10 p. 687 - 699
