N-[(1R,2S)-1-[(4R,7S)-5,8-二氧代-7-丙-2-基-12,15,18-三氧杂-3,6,9-三氮杂双环[17.3.1]二十三碳-1(23),19,21-三烯-4-基]-1-羟基-3-苯基丙烷-2-基]氨基甲酸叔丁酯合成路线 （共 2 条）
反应条件
1: 1-hydroxybenzotriazole, N-ethyl-N'-(3-(dimethylamino)propyl)carbodiimide hydrochloride / dimethylformamide / 24 h / Ambient temperature 2: pyridine / CH2Cl2 / 12 h / 0 - 20 °C 3: K2CO3, tetrabutylammonium iodide / dimethylsulfoxide / 4 h / 70 °C 4: hydroxyammonium chloride, aq. AcONa / ethanol / 1.5 h / 60 °C 5: formic acid, H2 / 10percent Pd/C / methanol / 3 h / 760 Torr 6: ethanol / 24 h / 80 °C 7: 0.4 M aq. LiOH / dioxane / 16 h / Ambient temperature 8: 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine, N-ethyl-N'-(3-(dimethylamino)propyl)carbodiimide hydrochloride / tetrahydrofuran / 120 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 39, # 17 p. 3291 - 3299
反应条件
1: 1-hydroxybenzotriazole, N-ethyl-N'-(3-(dimethylamino)propyl)carbodiimide hydrochloride / dimethylformamide / 24 h / Ambient temperature 2: pyridine / CH2Cl2 / 12 h / 0 - 20 °C 3: K2CO3, tetrabutylammonium iodide / dimethylsulfoxide / 4 h / 70 °C 4: hydroxyammonium chloride, aq. AcONa / ethanol / 1.5 h / 60 °C 5: formic acid, H2 / 10percent Pd/C / methanol / 3 h / 760 Torr 6: ethanol / 24 h / 80 °C 7: 0.4 M aq. LiOH / dioxane / 16 h / Ambient temperature 8: 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine, N-ethyl-N'-(3-(dimethylamino)propyl)carbodiimide hydrochloride / tetrahydrofuran / 120 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 39, # 17 p. 3291 - 3299
