5-氨基-2,3-二氢-1H-茚-1-羧酸合成路线 （共 6 条）
反应条件
1: With perchloric acid; hydrogen; acetic acid; palladium 10 on activated carbon
T=20°C; P=3000.3 Torr; 8 h;
2: With ammonia in water
T=0°C;
3: With hydrogenchloride in water
T=20°C; pH=4;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GMBH
Patent: WO2006/108640 A1, 2006 ;
Location in patent: Page/Page column 77 ;
WO 2006/108640 A1
反应条件
hydrogenchloride; water
48 h; Reflux;
参考文献
MERCK SHARP and DOHME CORP.; TANG, Haifeng; PIO, Barbara; TEUMELSAN, Nardos; PASTERNAK, Alexander; DEJESUS, Reynalda
Patent: WO2013/62892 A1, 2013 ;
Location in patent: Page/Page column 45 ;
反应条件
1: triethylamine / dichloromethane / 0.5 h / 0 - 20 °C
2: acetic anhydride; chromium(VI) oxide / water; acetic acid / 10 °C
3: sodium methylate / methanol; ethylene glycol dimethyl ether / 20 °C / |Cooling with ice
4: hydrogenchloride; water / 48 h / |Reflux
View Scheme
参考文献
MERCK SHARP and DOHME CORP.; TANG, Haifeng; PIO, Barbara; TEUMELSAN, Nardos; PASTERNAK, Alexander; DEJESUS, Reynalda
Patent: WO2013/62892 A1, 2013 ;
反应条件
1: acetic anhydride; chromium(VI) oxide / water; acetic acid / 10 °C
2: sodium methylate / methanol; ethylene glycol dimethyl ether / 20 °C / |Cooling with ice
3: hydrogenchloride; water / 48 h / |Reflux
View Scheme
参考文献
MERCK SHARP and DOHME CORP.; TANG, Haifeng; PIO, Barbara; TEUMELSAN, Nardos; PASTERNAK, Alexander; DEJESUS, Reynalda
Patent: WO2013/62892 A1, 2013 ;
反应条件
1: sodium methylate / methanol; ethylene glycol dimethyl ether / 20 °C / |Cooling with ice
2: hydrogenchloride; water / 48 h / |Reflux
View Scheme
参考文献
MERCK SHARP and DOHME CORP.; TANG, Haifeng; PIO, Barbara; TEUMELSAN, Nardos; PASTERNAK, Alexander; DEJESUS, Reynalda
Patent: WO2013/62892 A1, 2013 ;
反应条件
1: With sulfuric acid
T=80°C; 4 h;
2: With sodium hydroxide in water; ethyl acetate
T=20°C;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GMBH
Patent: WO2006/108640 A1, 2006 ;
Location in patent: Page/Page column 77 ;
WO 2006/108640 A1
