[(1S,2R)-1-苄基-2-羟基-3-[异丁基[(4-硝基苯基)磺酰]氨基]丙基]氨基甲酸叔丁酯合成路线 (共 23 条)
反应条件
1: Bu4NF / tetrahydrofuran 2: 90 percent / propan-2-ol / 5 h / 50 °C 3: 88 percent / Et3N / CH2Cl2 / 12 h / 20 °C View Scheme
参考文献
Organic letters, , vol. 3, # 15 p. 2349 - 2351
反应条件
1.1: TBAF / tetrahydrofuran / 0.67 h / 20 °C 1.2: 75 percent / KOH / methanol / 2 h / 20 °C 2.1: 90 percent / propan-2-ol / 5 h / 50 °C 3.1: 88 percent / Et3N / CH2Cl2 / 12 h / 20 °C View Scheme
参考文献
Organic letters, , vol. 3, # 15 p. 2349 - 2351
反应条件
1.1: sodium hydrogencarbonate / dichloromethane / 5 h / Reflux 2.1: triethylamine / dichloromethane / Reflux 2.2: Reflux View Scheme
反应条件
1: isopropyl alcohol / 6 h / 80 °C 2: triethylamine / dichloromethane / 12 h / 0 - 20 °C View Scheme
反应条件
1: 1,4-dioxane / 1 h / 10 - 25 °C 2: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 1,4-dioxane / 6 h / 80 - 85 °C View Scheme
参考文献
WO2013/11485 A1, ;
WO 2013/011485 A1
反应条件
1: sodium carbonate / water / 3 h / 60 - 65 °C 2: triethylamine / dichloromethane / 40 - 45 °C View Scheme
反应条件
1: hydrogenchloride 2: aluminum isopropoxide / isopropyl alcohol / 3 h / |Reflux 3: sodium carbonate / water / 3 h / 60 - 65 °C 4: triethylamine / dichloromethane / 40 - 45 °C View Scheme
反应条件
1: aluminum isopropoxide / isopropyl alcohol / 3 h / |Reflux 2: sodium carbonate / water / 3 h / 60 - 65 °C 3: triethylamine / dichloromethane / 40 - 45 °C View Scheme
反应条件
hydrogenchloride in 1,4-dioxane T=0 - 20°C;
参考文献
AMPLYX PHARMACEUTICALS, INC.; MUTZ, Mitchell; BARR, Kenneth, J.; GESTWICKI, Jason
Patent: WO2010/77317 A2, 2010 ;
Location in patent: Page/Page column 108; 109 ;
WO 2010/077317 A2
反应条件
1.1: hydrogen; triethanolamine / palladium 10 on activated carbon / methanol / 2 h / 40 - 45 °C 2.1: hydrogenchloride; water / 2 h / Reflux 3.1: 1-methyl-pyrrolidin-2-one / 10 h / -4 - 30 °C 3.2: 1 h / 45 - 50 °C View Scheme
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 ;