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: 79 percent / Et3N / CH2Cl2 / 4 h / 20 °C 2: 95 percent / H2 / Pd/C / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 48, # 6 p. 1813 - 1822
反应条件
1: 86 percent / KF; O(9)-benzyl-N-(9-anthracenylmethyl)cinchonidium fluoride / tetrahydrofuran / 6 h / -10 °C 2: 85 percent / NaBH4; NiCl2 / methanol / 0.17 h / 0 °C 3: MgSO4 4: NaBH4 / ethanol / 4 h / 0 - 23 °C 5: 94 percent / Et3N / CH2Cl2 / 2 h / 23 °C 6: H2 / Pd(OH)2/C / methanol / 4 h / 23 °C View Scheme
参考文献
Angewandte Chemie - International Edition, , vol. 38, # 13-14 p. 1931 - 1934
反应条件
1: 85 percent / NaBH4; NiCl2 / methanol / 0.17 h / 0 °C 2: MgSO4 3: NaBH4 / ethanol / 4 h / 0 - 23 °C 4: 94 percent / Et3N / CH2Cl2 / 2 h / 23 °C 5: H2 / Pd(OH)2/C / methanol / 4 h / 23 °C View Scheme
参考文献
Angewandte Chemie - International Edition, , vol. 38, # 13-14 p. 1931 - 1934
反应条件
1: MgSO4 2: NaBH4 / ethanol / 4 h / 0 - 23 °C 3: 94 percent / Et3N / CH2Cl2 / 2 h / 23 °C 4: H2 / Pd(OH)2/C / methanol / 4 h / 23 °C View Scheme
参考文献
Angewandte Chemie - International Edition, , vol. 38, # 13-14 p. 1931 - 1934
反应条件
1: 75 percent / Et3N / CH2Cl2 / 0 - 20 °C 2: 70 percent / H2 / Pd/C / ethyl acetate View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 11, # 22 p. 4769 - 4777
反应条件
1: 75 percent / Et3N / CH2Cl2 / 0 - 20 °C 2: 70 percent / H2 / Pd/C / ethyl acetate View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 11, # 22 p. 4769 - 4777
反应条件
1: propan-2-ol / 12 h / 80 °C 2: aq. NaHCO3 3: H2 / 10percent Pd/C / ethyl acetate View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 8, # 6 p. 687 - 690
反应条件
1: aq. NaHCO3 2: H2 / 10percent Pd/C / ethyl acetate View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 8, # 6 p. 687 - 690
反应条件
1.1: sodium hydrogencarbonate / dichloromethane / 5 h / Reflux 2.1: triethylamine / dichloromethane / Reflux 2.2: Reflux 3.1: hydrogen; triethanolamine / palladium 10 on activated carbon / methanol / 2 h / 40 - 45 °C 3.2: 2 h / Reflux 3.3: 10 h / 20 °C / pH 9 - 10 View Scheme
反应条件
1.1: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 1,4-dioxane / 14 h / 85 - 90 °C 2.1: hydrogenchloride; water / ethanol / 10 h / 55 - 65 °C 2.2: 0.5 h / 25 - 30 °C / pH 11.5 - 12.5 View Scheme
参考文献
WO2013/11485 A1, ;
WO 2013/011485 A1
