4-氨基-N-[(2R, 3S)-3-氨基-2-羟基-4-苯丁基]-N-异丁基苯磺酰胺合成路线 （共 30 条）
反应条件
1.1: 1,4-dioxane / 3.58 h / 5 - 25 °C 2.1: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 1,4-dioxane / 14 h / 85 - 90 °C 3.1: hydrogenchloride; water / ethanol / 10 h / 55 - 65 °C 3.2: 0.5 h / 25 - 30 °C / pH 11.5 - 12.5 View Scheme
参考文献
WO2013/11485 A1, ;
WO 2013/011485 A1
反应条件
1.1: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 1,4-dioxane / 6 h / 80 - 85 °C 2.1: trifluoroacetic acid / dichloromethane / 2 h / 20 - 25 °C 2.2: pH 8.5 - 9.2 3.1: hydrogen; palladium 10 on activated carbon / ethanol / 0.58 h / 20 - 25 °C / 2068.65 Torr View Scheme
参考文献
WO2013/11485 A1, ;
WO 2013/011485 A1
反应条件
1.1: 1,4-dioxane / 0.83 h / 5 - 25 °C 2.1: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 1,4-dioxane / 6 h / 80 - 85 °C 3.1: trifluoroacetic acid / dichloromethane / 2 h / 20 - 25 °C 3.2: pH 8.5 - 9 View Scheme
参考文献
WO2013/11485 A1, ;
WO 2013/011485 A1
反应条件
1.1: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 1,4-dioxane / 6 h / 80 - 85 °C 2.1: trifluoroacetic acid / dichloromethane / 2 h / 20 - 25 °C 2.2: pH 8.5 - 9 View Scheme
参考文献
WO2013/11485 A1, ;
WO 2013/011485 A1
反应条件
1.1: sodium carbonate / water / 3 h / 60 - 65 °C 2.1: triethylamine / dichloromethane / 40 - 45 °C 3.1: palladium 10 on activated carbon; hydrogen; triethanolamine / isopropyl alcohol / 3 h / 40 - 45 °C / 3000.3 - 4500.45 Torr 3.2: |Reflux View Scheme
反应条件
1.1: hydrogenchloride 2.1: aluminum isopropoxide / isopropyl alcohol / 3 h / |Reflux 3.1: sodium carbonate / water / 3 h / 60 - 65 °C 4.1: triethylamine / dichloromethane / 40 - 45 °C 5.1: palladium 10 on activated carbon; hydrogen; triethanolamine / isopropyl alcohol / 3 h / 40 - 45 °C / 3000.3 - 4500.45 Torr 5.2: |Reflux View Scheme
反应条件
1.1: aluminum isopropoxide / isopropyl alcohol / 3 h / |Reflux 2.1: sodium carbonate / water / 3 h / 60 - 65 °C 3.1: triethylamine / dichloromethane / 40 - 45 °C 4.1: palladium 10 on activated carbon; hydrogen; triethanolamine / isopropyl alcohol / 3 h / 40 - 45 °C / 3000.3 - 4500.45 Torr 4.2: |Reflux View Scheme
反应条件
1: (3R,3aS,6aR)-hexahydrofuro [2,3-b]furan-3-yl 4-nitrophenyl carbonate; 4-amino-N-(2R,3S)-(3-amino-2-hydroxy-4-phenylbutyl)-N-isobutyl-benzene sulfonamide in 1-methyl-pyrrolidin-2-one T=-4 - 30°C; 10 h; 2: ethanol T=45 - 50°C; 1 h;
参考文献
Vellanki, Siva Rama Prasad; Sahu, Arabinda; Katukuri, Aravind Kumar; Vanama, Vikram; Kothari, Satishbabu; Ponnekanti, Venkata Suryanarayana; Datta, Debashish
Patent: US2012/251826 A1, 2012 ;
Location in patent: Page/Page column 10 ;
反应条件
triethylamine in tetrahydrofuran 16 h;
参考文献
G. D. Searle and Co.
Patent: US6388132 B1, 2002 ;
Location in patent: Page column 84 ;
反应条件
triethylamine in tetrahydrofuran; dichloromethane
参考文献
G. D. Searle and Co.
Patent: US6172101 B2, 2001 ;
US 6172101 B1
