3(S)-羟基甲基-4-苄基吗啉合成路线 （共 5 条）
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
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 3: 1) borane-dimethylsulphide complex, triethylamine; 2) aq. sodium hydroxide (2M) / 1) THF, 0 deg C, 15 min; 2) reflux, 6 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: 23 percent / sodium hydroxide / H2O / 0 deg C, 30 min, 30-33 deg C, 2 h 2: 1) borane-dimethylsulphide complex, triethylamine; 2) aq. sodium hydroxide (2M) / 1) THF, 0 deg C, 15 min; 2) reflux, 6 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
hydrogen; palladium 10 on activated carbon in methanol P=2585.81 Torr; 18 h;
参考文献
UCB PHARMA S.A.
Patent: WO2009/1089 A1, 2008 ;
Location in patent: Page/Page column 29-30 ;
WO 2009/001089 A1
反应条件
1: 1.) NaH / 1.) DMF, 40 deg C, 2.) DMF, from 80 deg C to 85 deg C, 7 h 2: 77 percent / NaHCO3 / CH2Cl2 / 16 h / Ambient temperature 3: KOH / H2O / 16 h / Heating View Scheme
参考文献
Brown; Foubister; Forster; Stribling
Journal of Medicinal Chemistry, 1986 , vol. 29, # 7 p. 1288 - 1290
