(E)-4-羟基他莫昔芬合成路线 （共 15 条）
反应条件
in tetrahydrofuran T=60°C; 43 h;
参考文献
THE REGENTS OF THE UNIVERSITY OF COLORADO
Patent: WO2005/34856 A2, 2005 ;
Location in patent: Page/Page column 94 ;
反应条件
hydrogenchloride in methanol T=60 - 70°C; 0.5 h; Yield given. Yields of byproduct given;
参考文献
Foster; Jarman; Leung; McCague; Leclercq; Devleeschouwer
Journal of Medicinal Chemistry, 1985 , vol. 28, # 10 p. 1491 - 1497
反应条件
1.1: 91 percent / TiCl4; Zn / tetrahydrofuran / 2 h / Heating 2.1: Cs2CO3 / dimethylformamide / 0.17 h / 70 - 80 °C 2.2: dimethylformamide / 1.5 h / 70 - 80 °C View Scheme
参考文献
Chu, Guo-Hua; Peters, Amy; Selcer, Kyle W.; Li, Pui-Kai
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 141 - 144
反应条件
in ethanol T=60°C; 168 h; Reactivity;
参考文献
LABORATOIRES BESINS INTERNATIONAL
Patent: EP1579857 A1, 2005 ;
Location in patent: Page/Page column 11; 12 ;
反应条件
1: 4-(1-(4-hydroxylphenyl)-2-phenylbut-1-enyl)phenol With caesium carbonate in N,N-dimethyl-formamide T=70 - 80°C; 0.166667 h; 2: 2-dimethylamino-1-chloro-ethane hydrochloride in N,N-dimethyl-formamide T=70 - 80°C; 1.5 h;
参考文献
Yu, Donna D.; Forman, Barry M.
Journal of Organic Chemistry, 2003 , vol. 68, # 24 p. 9489 - 9491
反应条件
1: Zn, TiCl4 / tetrahydrofuran 2: H2 / Pd/C / 2 h / Ambient temperature View Scheme
参考文献
Chu, Guo-Hua; Peters, Amy; Selcer, Kyle W.; Li, Pui-Kai
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 141 - 144
反应条件
1: 1.) n-butyllithium / 1.) hexane, THF, -78 deg C, 30 min, 2.) hexane, THF, RT, 10 h 2: conc. aq. HCl / methanol / 0.5 h / 60 - 70 °C View Scheme
参考文献
Foster; Jarman; Leung; McCague; Leclercq; Devleeschouwer
Journal of Medicinal Chemistry, 1985 , vol. 28, # 10 p. 1491 - 1497
反应条件
1: toluene-p-sulfonic acid / 1 h / Ambient temperature 2: 1.) n-butyllithium / 1.) hexane, THF, -78 deg C, 30 min, 2.) hexane, THF, RT, 10 h 3: conc. aq. HCl / methanol / 0.5 h / 60 - 70 °C View Scheme
参考文献
Foster; Jarman; Leung; McCague; Leclercq; Devleeschouwer
Journal of Medicinal Chemistry, 1985 , vol. 28, # 10 p. 1491 - 1497
反应条件
1.1: 91 percent / TiCl4; Zn / tetrahydrofuran / 2 h / Heating 2.1: Cs2CO3 / dimethylformamide / 0.17 h / 70 - 80 °C 2.2: dimethylformamide / 1.5 h / 70 - 80 °C View Scheme
参考文献
Gauthier, Sylvain; Mailhot, Josee; Labrie, Fernand
Journal of Organic Chemistry, 1996 , vol. 61, # 11 p. 3890 - 3893
反应条件
hydrogen; palladium on activated charcoal 2 h; Ambient temperature;
参考文献
Chu, Guo-Hua; Peters, Amy; Selcer, Kyle W.; Li, Pui-Kai
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 141 - 144
