1-(7-氨基-3,4-二氢-2(1h)-异喹啉)乙酮合成路线 （共 10 条）
反应条件
1.1: 94 percent / TFA / CH2Cl2 / 0.25 h / Heating 2.1: H2SO4; KNO3 / 0 °C 2.2: 1.1 g / aq. HCl / methanol / 0.83 h / Heating 3.1: aq. NaNO2; aq. HCl / 2 h / 0 °C 3.2: 65 percent / aq. H3PO2 / 10 h / 40 °C 4.1: aq. HCl / methanol / 10 h / Heating View Scheme
参考文献
Zhu, Zhengxiang; Furr, John; Buolamwini, John K.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 831 - 837
反应条件
1: 1.) aq. HCl, aq. NaNO2, 2.) aq. KI / 1.) 30 min, 2.) CHCl3, RT, 7 h 2: 78 percent / CuI, KF / dimethylformamide / 8 h / Heating 3: 67 percent / 3 N HCl / ethanol / 4 h / Heating View Scheme
参考文献
Grunewald, Gary L.; Dahanukar, Vilas H.; Jalluri, Ravi K.; Criscione, Kevin R.
Journal of Medicinal Chemistry, 1999 , vol. 42, # 1 p. 118 - 134
反应条件
hydrogenchloride; hydrogen; platinum (IV) oxide in ethanol; water
P=2068.65 Torr;
参考文献
SMITHKLINE BEECHAM CORPORATION
Patent: WO2005/16914 A1, 2005 ;
Location in patent: Page/Page column 81-82 ;
WO 2005/016914 A1
参考文献
SmithKline Corporation
Patent: US4321254 A1, 1982 ;
反应条件
1.1: 50 percent / KNO3; H2SO4 / 5 - 20 °C
2.1: 94 percent / Et3N / CH2Cl2 / 1 h / Heating
3.1: FeCl3*6H2O; activated carbon / methanol / 0.33 h / Heating
3.2: 85 percent / NH2NH2*H2O / methanol / 4 h / Heating
View Scheme
参考文献
Zhu, Zhengxiang; Furr, John; Buolamwini, John K.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 831 - 837
反应条件
1.1: 94 percent / Et3N / CH2Cl2 / 1 h / Heating
2.1: FeCl3*6H2O; activated carbon / methanol / 0.33 h / Heating
2.2: 85 percent / NH2NH2*H2O / methanol / 4 h / Heating
View Scheme
参考文献
Zhu, Zhengxiang; Furr, John; Buolamwini, John K.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 831 - 837
反应条件
1: aqueous nitric acid; sulfuric acid
2: palladium/charcoal; ethanol / Hydrogenation
View Scheme
参考文献
Ochiai; Nakagome
Chemical and Pharmaceutical Bulletin, 1958 , vol. 6, p. 497,500
反应条件
1: sodium acetate
2: palladium/charcoal; ethanol / Hydrogenation
View Scheme
参考文献
Ochiai; Nakagome
Chemical and Pharmaceutical Bulletin, 1958 , vol. 6, p. 497,500
反应条件
1: 1.) aq. HCl, aq. NaNO2, 2.) aq. KI / 1.) 30 min, 2.) CHCl3, RT, 7 h
2: 87 percent / 3 N HCl / ethanol / 4 h / Heating
View Scheme
参考文献
Grunewald, Gary L.; Dahanukar, Vilas H.; Jalluri, Ravi K.; Criscione, Kevin R.
Journal of Medicinal Chemistry, 1999 , vol. 42, # 1 p. 118 - 134
反应条件
1.1: 94 percent / TFA / CH2Cl2 / 0.25 h / Heating
2.1: H2SO4; KNO3 / 0 °C
2.2: 0.5 g / aq. HCl / methanol / 0.83 h / Heating
3.1: aq. NaNO2; aq. HCl / 2 h / 0 °C
3.2: 86 percent / aq. H3PO2 / 10 h / 40 °C
4.1: aq. HCl / methanol / 10 h / Heating
View Scheme
参考文献
Zhu, Zhengxiang; Furr, John; Buolamwini, John K.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 831 - 837
