3-[[(1R)-2-[[(2R)-2-(2-金刚烷基氧基羰基氨基)-3-(1H-吲哚-3-基)-2-甲基-丙酰]氨基]-1-苯基-乙基]氨基甲酰]丙酸合成路线 (共 11 条)
反应条件
1: 100 percent / pyridine / CH2Cl2 / 2 h / Ambient temperature 2: 89 percent / Et3N / tetrahydrofuran / 0.25 h 3: 90 percent / LiOH / H2O; dioxane / 18 h / Ambient temperature 4: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 5: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 6: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: 87 percent / Et3N / tetrahydrofuran / 18 h / Ambient temperature 2: Et3N / CH2Cl2 / 18 h / Ambient temperature 3: NaN3 / dimethylformamide / 3 h / 80 °C 4: Lindlar catalyst, H2 / ethyl acetate / 6 h / 30 °C / 2327.2 Torr 5: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 6: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 7: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: 89 percent / Et3N / tetrahydrofuran / 0.25 h 2: 90 percent / LiOH / H2O; dioxane / 18 h / Ambient temperature 3: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 4: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 5: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 2: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 2: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 3: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: Et3N / CH2Cl2 / 18 h / Ambient temperature 2: NaN3 / dimethylformamide / 3 h / 80 °C 3: Lindlar catalyst, H2 / ethyl acetate / 6 h / 30 °C / 2327.2 Torr 4: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 5: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 6: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: Lindlar catalyst, H2 / ethyl acetate / 6 h / 30 °C / 2327.2 Torr 2: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 3: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 4: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 2: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 3: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: NaN3 / dimethylformamide / 3 h / 80 °C 2: Lindlar catalyst, H2 / ethyl acetate / 6 h / 30 °C / 2327.2 Torr 3: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 4: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 5: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414
反应条件
1: 90 percent / LiOH / H2O; dioxane / 18 h / Ambient temperature 2: 1.) 1-hydroxybenzotriazole hydrate, N,N'-dicyclohexylcarbodiimide / 1.) EtOAc, RT, 2 h, 2.) 18 h 3: 89 percent / H2 / Pearlman's catalyst / ethanol / 18 h / 25 °C / 2327.2 Torr 4: 80 percent / ethyl acetate / 24 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 1 p. 404 - 414