N-Boc-4,4-二氟环已胺合成路线 （共 13 条）
反应条件
thionyl chloride in methanol T=20°C; 0.5 h;
参考文献
WO2004/111033 A1, ;
Page 24; 25 ;
WO 2004/111033 A1
反应条件
hydrogenchloride T=20°C;
参考文献
AGIOS PHARMACEUTICALS, INC.; LEMIEUX, Rene M.; POPOVICI-MULLER, Janeta; TRAVINS, Jeremy; CAI, Zhenwei; CUI, Dawei; ZHOU, Ding
Patent: WO2013/107291 A1, 2013 ;
Location in patent: Page/Page column 65 ;
反应条件
hydrogenchloride in 1,4-dioxane T=20°C; 3 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2004/24728 A2, 2004 ;
Location in patent: Page 113 ;
WO 2004/024728 A2
反应条件
diethylamino-sulfur trifluoride in dichloromethane
15 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2004/50619 A1, 2004 ;
Location in patent: Page 71 ;
WO 2004/050619 A1
反应条件
diethylamino-sulfur trifluoride in dichloromethane
T=-5 - 20°C; Inert atmosphere;
参考文献
AGIOS PHARMACEUTICALS, INC.; LEMIEUX, Rene M.; POPOVICI-MULLER, Janeta; TRAVINS, Jeremy; CAI, Zhenwei; CUI, Dawei; ZHOU, Ding
Patent: WO2013/107291 A1, 2013 ;
Location in patent: Page/Page column 64 ;
反应条件
triethylamine in dichloromethane
T=20 - 50°C; 5 h;
参考文献
sanofi-aventis
Patent: US2008/269170 A1, 2008 ;
Location in patent: Page/Page column 62 ;
反应条件
sodium tetrahydroborate; diethylamino-sulfur trifluoride; 3-chloro-benzenecarboperoxoic acid in methanol; water; ethyl acetate; Petroleum ether
参考文献
AGIOS PHARMACEUTICALS, INC; Lemieux, Rene M.; Popovici-Muller, Janeta; Travins, Jeremy; Cai, Zhenwei; Cui, Dawei; Zhou, Ding
Patent: US2013/190249 A1, 2013 ;
Location in patent: Page/Page column ;
反应条件
1: triethylamine / methanol; tetrahydrofuran
2: Petroleum ether; ethyl acetate
3: diethylamino-sulfur trifluoride; sodium tetrahydroborate; 3-chloro-benzenecarboperoxoic acid / Petroleum ether; ethyl acetate; methanol; water
View Scheme
参考文献
AGIOS PHARMACEUTICALS, INC; Lemieux, Rene M.; Popovici-Muller, Janeta; Travins, Jeremy; Cai, Zhenwei; Cui, Dawei; Zhou, Ding
Patent: US2013/190249 A1, 2013 ;
反应条件
1: Petroleum ether; ethyl acetate
2: diethylamino-sulfur trifluoride; sodium tetrahydroborate; 3-chloro-benzenecarboperoxoic acid / Petroleum ether; ethyl acetate; methanol; water
View Scheme
参考文献
AGIOS PHARMACEUTICALS, INC; Lemieux, Rene M.; Popovici-Muller, Janeta; Travins, Jeremy; Cai, Zhenwei; Cui, Dawei; Zhou, Ding
Patent: US2013/190249 A1, 2013 ;
反应条件
1.1: triethylamine / tetrahydrofuran / 20 °C
2.1: Dess-Martin periodane / dichloromethane / 20 °C
3.1: diethylamino-sulfur trifluoride / dichloromethane / -5 - 20 °C / |Inert atmosphere
3.2: 0 - 20 °C
3.3: 0 - 20 °C
View Scheme
参考文献
AGIOS PHARMACEUTICALS, INC.; LEMIEUX, Rene M.; POPOVICI-MULLER, Janeta; TRAVINS, Jeremy; CAI, Zhenwei; CUI, Dawei; ZHOU, Ding
Patent: WO2013/107291 A1, 2013 ;
