(R)-N-Boc-3-四氢吡咯乙酸合成路线 （共 6 条）
反应条件
in dimethyl sulfoxide; toluene 2 h; Reflux; Product distribution / selectivity;
参考文献
TARGACEPT, INC.; TOLER, Steven M.; HOSFORD, David A.; LIPPIELLO, Patrick M.; DUNBAR, Geoffrey Charles; CALDWELL, William Scott; HAMEDANI, Parviz; BENCHERIF, Merouane
Patent: WO2011/112428 A2, 2011 ;
Location in patent: Page/Page column 32 ;
反应条件
sodium hydroxide; trifluoroacetic acid in 1,4-dioxane; dichloromethane
反应条件
1.1: potassium tert-butylate / 1-methyl-pyrrolidin-2-one / 35 - 40 °C 1.2: 18 h / 65 °C 1.3: pH 3 - 4 2.1: diethyl malonate; potassium hydroxide / water; tetrahydrofuran / 25 - 45 °C 2.2: 0.5 h / 5 - 10 °C 3.1: dimethyl sulfoxide / toluene / 2 h / Reflux View Scheme
反应条件
1.1: diethyl malonate; potassium hydroxide / water; tetrahydrofuran / 25 - 45 °C 1.2: 0.5 h / 5 - 10 °C 2.1: dimethyl sulfoxide / toluene / 2 h / Reflux View Scheme
反应条件
1: ((3R)-1-{[(1,1-dimethylethyl)oxy]carbonyl}-3-pyrrolidinyl)acetic acid With hydrogenchloride in 1,4-dioxane T=18 - 25°C; 20 h; 2: methanol With hydrogenchloride T=10 - 25°C;
参考文献
AstraZeneca AB
Patent: US2008/269288 A1, 2008 ;
Location in patent: Page/Page column 105 ;
US 20080269288 A1
反应条件
1.1: borane-THF / tetrahydrofuran / 2.75 h / 23 - 28 °C / Inert atmosphere 1.2: 1.67 h / 10 - 25 °C 2.1: triethylamine / toluene / -10 - 20 °C 3.1: sodium iodide / ethylene glycol dimethyl ether / 4 h / 50 - 60 °C 3.2: -10 - 20 °C View Scheme
参考文献
TARGACEPT, INC.; TOLER, Steven M.; HOSFORD, David A.; LIPPIELLO, Patrick M.; DUNBAR, Geoffrey Charles; CALDWELL, William Scott; HAMEDANI, Parviz; BENCHERIF, Merouane
Patent: WO2011/112428 A2, 2011 ;
