(2S,6R)-6-[[(1S)-1-乙氧羰基]-3-苯基丙基]氨基-2-(2-噻吩基)-1,4-硫氮杂卓-5-酮合成路线 (共 12 条)
反应条件
triethylamine in dichloromethane 16 h; Ambient temperature;
参考文献
Yanagisawa, Hiroaki; Ishihara, Sadao; Ando, Akiko; Kanazaki, Takuro; Miyamoto, Shuichi; et al.
Journal of Medicinal Chemistry, 1987 , vol. 30, # 11 p. 1984 - 1991
反应条件
1: N-methylmorpholine / toluene / 16 h / Ambient temperature 2: 64 percent / H2, AcOH / 5percent Pd/C / 5 h / 70 °C / 2280 Torr 3: 69 percent / diphenyl phosphorazidate, N-methylmorpholine / dimethylformamide / 16 h / Ambient temperature 4: 35 percent / 4 N aq. HCl / dioxane / 4 h / Ambient temperature 5: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 100 percent / p-toluenesulfonic acid*H2O / benzene / 5 h / Heating 2: 29 percent / H2 / 5percent Pd/C / propan-2-ol / 5 h / 50 °C / 2280 Torr 3: 86 percent / KOH / ethanol / 16 h / Ambient temperature 4: 98 percent / conc. H2SO4 / 16 h / Ambient temperature 5: 100 percent / pyridine / CH2Cl2 / 0.5 h / 0 °C 6: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 29 percent / H2 / 5percent Pd/C / propan-2-ol / 5 h / 50 °C / 2280 Torr 2: 86 percent / KOH / ethanol / 16 h / Ambient temperature 3: 98 percent / conc. H2SO4 / 16 h / Ambient temperature 4: 100 percent / pyridine / CH2Cl2 / 0.5 h / 0 °C 5: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 64 percent / H2, AcOH / 5percent Pd/C / 5 h / 70 °C / 2280 Torr 2: 69 percent / diphenyl phosphorazidate, N-methylmorpholine / dimethylformamide / 16 h / Ambient temperature 3: 35 percent / 4 N aq. HCl / dioxane / 4 h / Ambient temperature 4: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 86 percent / KOH / ethanol / 16 h / Ambient temperature 2: 98 percent / conc. H2SO4 / 16 h / Ambient temperature 3: 100 percent / pyridine / CH2Cl2 / 0.5 h / 0 °C 4: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 98 percent / conc. H2SO4 / 16 h / Ambient temperature 2: 100 percent / pyridine / CH2Cl2 / 0.5 h / 0 °C 3: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 100 percent / pyridine / CH2Cl2 / 0.5 h / 0 °C 2: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 35 percent / 4 N aq. HCl / dioxane / 4 h / Ambient temperature 2: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991
反应条件
1: 69 percent / diphenyl phosphorazidate, N-methylmorpholine / dimethylformamide / 16 h / Ambient temperature 2: 35 percent / 4 N aq. HCl / dioxane / 4 h / Ambient temperature 3: 80 percent / Et3N / CH2Cl2 / 16 h / Ambient temperature View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 11 p. 1984 - 1991