4-甲基-4-羟基哌啶盐酸盐合成路线 （共 9 条）
反应条件
1: 4-methyl-piperidin-4-ol hydrochloride With sodium hydride; triethylamine in N,N-dimethyl-formamide; mineral oil T=25°C; 0.35 h; 2: di-tert-butyl dicarbonate in N,N-dimethyl-formamide; mineral oil T=25°C; 18 h;
参考文献
US2009/192156 A1, ;
Page/Page column 27-28 ;
反应条件
hydrogenchloride in 1,4-dioxane
T=0 - 23°C; 2 h;
参考文献
H. LUNDBECK A/S
Patent: US2011/92475 A1, 2011 ;
Location in patent: Page/Page column 19 ;
反应条件
1: With hydrogen; palladium 10 on activated carbon in methanol
P=1810.07 Torr; 18 h;
2: With hydrogenchloride in 1,4-dioxane; methanol
参考文献
EXELIXIS, INC.; RICE, Kenneth
Patent: WO2012/71509 A2, 2012 ;
Location in patent: Page/Page column 154 ;
WO 2012/071509 A2
反应条件
hydrogen; palladium 10 on activated carbon in methanol
T=20°C; 14 h;
参考文献
Takeda Pharmaceutical Company Limited
Patent: EP2392573 A1, 2011 ;
Location in patent: Page/Page column 41 ;
反应条件
hydrogenchloride in methanol; water
参考文献
Eisai Co., Ltd.
Patent: EP1522540 A1, 2005 ;
Location in patent: Page/Page column 53 ;
EP 1522540 A1
反应条件
1: in tetrahydrofuran; diethyl ether
T=0 - 20°C; 48 h;
2: With hydrogenchloride in 1,4-dioxane; methanol
0.5 h;
参考文献
CHIRON CORPORATION; GLAXOSMITHKLINE
Patent: WO2004/112793 A1, 2004 ;
Location in patent: Page/Page column 129 ;
反应条件
1.1: tetrahydrofuran / 14 h / 20 °C / Cooling with ice
1.2: Cooling with ice
2.1: hydrogen / palladium 10 on activated carbon / methanol / 14 h / 20 °C
View Scheme
参考文献
Takeda Pharmaceutical Company Limited
Patent: EP2392573 A1, 2011 ;
反应条件
1: diethyl ether; tetrahydrofuran / 18 h / 0 - 20 °C
2: hydrogen / palladium 10 on activated carbon / methanol / 18 h / 1810.07 Torr
View Scheme
参考文献
EXELIXIS, INC.; RICE, Kenneth
Patent: WO2012/71509 A2, 2012 ;
WO 2012/071509 A2
反应条件
1: diethyl ether; tetrahydrofuran / 6 h / -78 - 23 °C
2: hydrogenchloride / 1,4-dioxane / 2 h / 0 - 23 °C
View Scheme
参考文献
H. LUNDBECK A/S
Patent: US2011/92475 A1, 2011 ;
