(2R,4S)-4-氟-1,2-吡咯烷二羧酸-1-(1,1-二甲基乙基)酯合成路线 （共 4 条）
反应条件
1: With water; sodium hydroxide in tetrahydrofuran; methanol
2 h;
2: With hydrogenchloride in water
pH=3;
参考文献
COMENTIS, INC.; BILCER, Geoffrey, M.; LILLY, John, C.; SWANSON, Lisa, M.
Patent: WO2011/130383 A1, 2011 ;
Location in patent: Page/Page column 86 ;
WO 2011/130383 A1
反应条件
1.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / water; acetone
2.1: [bis(2-methoxyethyl)amino]-sulfur trifluoride / dichloromethane / 12 h / -78 - 20 °C
3.1: sodium hydroxide; water / tetrahydrofuran; methanol / 2 h
3.2: pH 3
View Scheme
参考文献
COMENTIS, INC.; BILCER, Geoffrey, M.; LILLY, John, C.; SWANSON, Lisa, M.
Patent: WO2011/130383 A1, 2011 ;
WO 2011/130383 A1
反应条件
1.1: [bis(2-methoxyethyl)amino]-sulfur trifluoride / dichloromethane / 12 h / -78 - 20 °C
2.1: sodium hydroxide; water / tetrahydrofuran; methanol / 2 h
2.2: pH 3
View Scheme
参考文献
COMENTIS, INC.; BILCER, Geoffrey, M.; LILLY, John, C.; SWANSON, Lisa, M.
Patent: WO2011/130383 A1, 2011 ;
WO 2011/130383 A1
反应条件
1.1: acetyl chloride / 8 h / Inert atmosphere; Reflux
2.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / water; acetone
3.1: [bis(2-methoxyethyl)amino]-sulfur trifluoride / dichloromethane / 12 h / -78 - 20 °C
4.1: sodium hydroxide; water / tetrahydrofuran; methanol / 2 h
4.2: pH 3
View Scheme
参考文献
COMENTIS, INC.; BILCER, Geoffrey, M.; LILLY, John, C.; SWANSON, Lisa, M.
Patent: WO2011/130383 A1, 2011 ;
WO 2011/130383 A1
