5-甲氧基-2-四氢萘胺合成路线 (共 10 条)
反应条件
hydrogen; palladium on activated charcoal in ethanol
T=45°C; P=2280 Torr; 1 h;
参考文献
Copinga, Swier; Tepper, Pieter G.; Grol, Cor J.; Horn, Alan S.; Dubocovich, Margarita L.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2891 - 2898
反应条件
ammonium acetate; sodium hydroxide; sodium cyanoborohydride in methanol; water; ethyl acetate; acetone
参考文献
Dr. Karl Thomae GmbH
Patent: US4584293 A1, 1986 ;
反应条件
1: p-TsOH / H2O; toluene
2: 1.) H2, 2.) H2 / 1.) PtO2, 2.) 10percent Pd/C / 1.) MeOH, 2.) MeOH
View Scheme
参考文献
van Vliet; Tepper; Dijkstra; Damsma; Wikstroem; Pugsley; Akunne; Heffner; Glase; Wise
Journal of medicinal chemistry, 1996 , vol. 39, # 21 p. 4233 - 4237
反应条件
hydrogenchloride
18 h; Heating;
参考文献
Ye, Qizhuang; Grunewald, Gary L.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 2 p. 478 - 486
反应条件
1: 2N aq. NaOH / 1.) 55 deg C, 2 h, 2.) reflux 2 h
2: 1.) Na, EtOH, 2.) 2N aq. HCl / 1.) reflux, 1 h, 2.) EtOH, reflux, 30 min
3: p-TsOH*H2O / benzene / 17 h / Heating
4: H2 / PtO2 / ethanol / 2.5 h / 1520 Torr
5: H2 / 10percent Pd/C / ethanol / 1 h / 45 °C / 2280 Torr
View Scheme
参考文献
Copinga, Swier; Tepper, Pieter G.; Grol, Cor J.; Horn, Alan S.; Dubocovich, Margarita L.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2891 - 2898
反应条件
1: 1.) Na, EtOH, 2.) 2N aq. HCl / 1.) reflux, 1 h, 2.) EtOH, reflux, 30 min
2: p-TsOH*H2O / benzene / 17 h / Heating
3: H2 / PtO2 / ethanol / 2.5 h / 1520 Torr
4: H2 / 10percent Pd/C / ethanol / 1 h / 45 °C / 2280 Torr
View Scheme
参考文献
Copinga, Swier; Tepper, Pieter G.; Grol, Cor J.; Horn, Alan S.; Dubocovich, Margarita L.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2891 - 2898
反应条件
1: 77 percent / sodium hydride / diethyl ether / 12 h / Ambient temperature
2: sodium nitrite, acetic acid / CH2Cl2 / 0.5 h / 0 °C
3: zinc, acetic acid / 2 h
4: 92 percent / H2, conc. H2SO4 / 5percent palladium on carbon / acetic acid / 4 h / 2585.7 Torr
5: 86 percent / 3 N aq. HCl / 18 h / Heating
View Scheme
参考文献
Ye, Qizhuang; Grunewald, Gary L.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 2 p. 478 - 486
反应条件
1: zinc, acetic acid / 2 h
2: 92 percent / H2, conc. H2SO4 / 5percent palladium on carbon / acetic acid / 4 h / 2585.7 Torr
3: 86 percent / 3 N aq. HCl / 18 h / Heating
View Scheme
参考文献
Ye, Qizhuang; Grunewald, Gary L.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 2 p. 478 - 486
反应条件
1: 92 percent / H2, conc. H2SO4 / 5percent palladium on carbon / acetic acid / 4 h / 2585.7 Torr
2: 86 percent / 3 N aq. HCl / 18 h / Heating
View Scheme
参考文献
Ye, Qizhuang; Grunewald, Gary L.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 2 p. 478 - 486
反应条件
lithium aluminium tetrahydride in tetrahydrofuran
8 h; Heating;
参考文献
Yao, Bin; Ji, Haitao; Cao, Yongbin; Zhou, Youjun; Zhu, Jue; Lue, Jiaguo; Li, Yaowu; Chen, Jun; Zheng, Canhui; Jiang, Yuanying; Liang, Rongmei; Tang, Hui
Journal of Medicinal Chemistry, 2007 , vol. 50, # 22 p. 5293 - 5300