2-(羟甲基)-4-苄基吗啉合成路线 (共 13 条)
反应条件
1: With formamide T=215°C; 3 h; Inert atmosphere; 2: With water T=50°C; 2 h; Reflux;
参考文献
SANOFI; Brollo, Maurice; Carry, Jean-Christophe; Certal, Victor; Didier, Eric; Doerflinger, Gilles; EL Ahmad, Youssef; Filoche-Romme, Bruno; Halley, Frank; Karlsson, Karl Andreas; Schio, Laurent; Thompson, Fabienne
Patent: US2013/274253 A1, 2013 ;
Location in patent: Paragraph 1825-1826 ;
反应条件
1: With chloroformic acid ethyl ester; triethylamine in tetrahydrofuran T=-10 - -5°C; 2: With methanol; sodium tetrahydroborate in tetrahydrofuran T=0 - 5°C;
参考文献
ABBOTT LABORATORIES
Patent: US2010/63022 A1, 2010 ;
Location in patent: Page/Page column 29 ;
US 20100063022 A1
反应条件
tetra(n-butyl)ammonium hydroxide in water T=55°C;
参考文献
Henegar, Kevin E.
Journal of Organic Chemistry, 2008 , vol. 73, # 9 p. 3662 - 3665
反应条件
1.1: LDA / tetrahydrofuran / 0.25 h / -80 °C 1.2: 52 percent / tetrahydrofuran / 0.5 h / -80 °C 2.1: 73 percent / LiAlH4 / diethyl ether / Heating View Scheme
参考文献
Dobrev, Alexander; Nechev, Lubomir; Ivanov, Christo; Bon, Maryse
Journal of Chemical Research, Miniprint, 1999 , # 3 p. 1001 - 1047
反应条件
1: 79 percent / H2SO4 / 0.5 h / 150 °C 2: 63 percent / aq. formamide / 5 h / Heating View Scheme
参考文献
SANOFI; Brollo, Maurice; Carry, Jean-Christophe; Certal, Victor; Didier, Eric; Doerflinger, Gilles; EL Ahmad, Youssef; Filoche-Romme, Bruno; Halley, Frank; Karlsson, Karl Andreas; Schio, Laurent; Thompson, Fabienne
Patent: US2013/274253 A1, 2013 ;
反应条件
1: 98 percent / 0.5 h / 40 °C 2: 79 percent / H2SO4 / 0.5 h / 150 °C 3: 63 percent / aq. formamide / 5 h / Heating View Scheme
参考文献
SANOFI; Brollo, Maurice; Carry, Jean-Christophe; Certal, Victor; Didier, Eric; Doerflinger, Gilles; EL Ahmad, Youssef; Filoche-Romme, Bruno; Halley, Frank; Karlsson, Karl Andreas; Schio, Laurent; Thompson, Fabienne
Patent: US2013/274253 A1, 2013 ;
反应条件
1: 95 percent / H2 / 10percent Pd-C / methanol / Ambient temperature 2: 96.4 percent / Et3N / CH2Cl2 / 10 h / Ambient temperature 3: 70 percent / pyridine / CH2Cl2 / 15 h / Ambient temperature 4: 73.5 percent / dimethylformamide / 17 h / 100 - 105 °C 5: 77.7 percent / LiAlH4 / tetrahydrofuran / 3 h / Ambient temperature 6: 73.4 percent / 0.5 N HCl / ethanol / 17 h / Heating View Scheme
参考文献
Kojima; Niigata; Fujikura; et al.
Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 9 p. 3766 - 3774
反应条件
1: 95 percent / H2 / 10percent Pd-C / methanol / Ambient temperature 2: 96.4 percent / Et3N / CH2Cl2 / 10 h / Ambient temperature 3: 70 percent / pyridine / CH2Cl2 / 15 h / Ambient temperature 4: 73.5 percent / dimethylformamide / 17 h / 100 - 105 °C 5: 77.7 percent / LiAlH4 / tetrahydrofuran / 3 h / Ambient temperature 6: 73.4 percent / 0.5 N HCl / ethanol / 17 h / Heating View Scheme
参考文献
Kojima; Niigata; Fujikura; et al.
Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 9 p. 3766 - 3774
反应条件
hydrogen; palladium on activated charcoal in methanol Ambient temperature;
参考文献
Kojima; Niigata; Fujikura; et al.
Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 9 p. 3766 - 3774
反应条件
palladium monocarbide in methanol
参考文献
US2004/192653 A1, ;
US 20040192653 A1