(R)-4-苄基-5-氧代-3-吗啉甲酸合成路线 (共 7 条)
反应条件
1: With potassium carbonate in tetrahydrofuran; water T=0 - 4°C; 2 h; Industry scale; 2: With sodium hydroxide in tetrahydrofuran; water T=3 - 10°C; pH=13 - 13.5; 4.83333 h; Industry scale; 3: With hydrogenchloride in water T=3 - 6°C; pH=< 2; Industry scale;
参考文献
WO2011/23733 A1, ;
Page/Page column 19-20 ;
反应条件
1: With potassium tert-butylate in tert-butyl alcohol T=110°C; 3 h; 2: With hydrogenchloride in water pH=1;
参考文献
US2008/255114 A1, ;
Page/Page column 31 ;
反应条件
1: With sodium hydroxide in water T=0 - 45°C; 4.5 h; 2: With hydrogenchloride in water T=10°C; pH=1;
参考文献
WO2009/1089 A1, ;
Page/Page column 28-29 ;
WO 2009/001089 A1
反应条件
1: 1) sodium hydroxide (2 M); 2) sodium borohydride / 1) 30 min; 2) 6-10 deg C 2: 23 percent / sodium hydroxide / H2O / 0 deg C, 30 min, 30-33 deg C, 2 h View Scheme
参考文献
Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), , p. 2577 - 2580
反应条件
1: 65 percent / pyridine, phenyl dichlorophosphate / 1,2-dimethoxy-ethane / 18 h 2: 60 percent / borane-dimethyl sulphide complex (10 M) / tetrahydrofuran / 18 h View Scheme
参考文献
Brown, George R.; Foubister, Alan J.; Wright, Brian
Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1985 , p. 2577 - 2580
反应条件
1.1: dimethylsulfide borane complex / tetrahydrofuran / 5 h / 35 - 40 °C / Industry scale 1.2: 40 °C / Industry scale 1.3: 2.25 h / 5 - 15 °C / Industry scale 2.1: hydrogen / 20 palladium(II) hydroxide on carbon / ethanol / 3 h / 20 - 30 °C / 2311.54 Torr / Industry scale View Scheme
参考文献
GLAXOSMITHKLINE LLC; CRAIG, Andrew, Simon; ISMAIL, Salima, Zarah; LAWRENCE, Ronnie, Maxwell
Patent: WO2011/23733 A1, 2011 ;
反应条件
dimethylsulfide borane complex; triethylamine in tetrahydrofuran 12 h; Heating / reflux;
参考文献
UCB PHARMA S.A.
Patent: WO2009/71895 A1, 2009 ;
Location in patent: Page/Page column 110 ;
WO 2009/071895 A1