3-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-5-乙酰胺合成路线 (共 8 条)
反应条件
1.1: 59 percent / potassium iodide / N,N-dimethyl-acetamide / 50 °C 2.1: tetrazole / dimethylformamide / 20 °C 2.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 3.1: 99 percent / HCl / dioxane / 20 - 45 °C 4.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1.1: 82 percent / HCl / dioxane; N,N-dimethyl-acetamide / 0.67 h / 90 °C 2.1: pentafluorophenyl trifluoroacetate; pyridine / dimethylformamide / 0.5 h / 20 °C 2.2: 94 percent / dimethylformamide / 20 - 90 °C 3.1: 59 percent / potassium iodide / N,N-dimethyl-acetamide / 50 °C 4.1: tetrazole / dimethylformamide / 20 °C 4.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 5.1: 99 percent / HCl / dioxane / 20 - 45 °C 6.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1.1: tetrazole / dimethylformamide / 20 °C 1.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 2.1: 99 percent / HCl / dioxane / 20 - 45 °C 3.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1: 99 percent / HCl / dioxane / 20 - 45 °C 2: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1.1: 70 percent / SOCl2; N,N-dimethylacetamide / 1 h / 85 °C 2.1: 82 percent / HCl / dioxane; N,N-dimethyl-acetamide / 0.67 h / 90 °C 3.1: pentafluorophenyl trifluoroacetate; pyridine / dimethylformamide / 0.5 h / 20 °C 3.2: 94 percent / dimethylformamide / 20 - 90 °C 4.1: 59 percent / potassium iodide / N,N-dimethyl-acetamide / 50 °C 5.1: tetrazole / dimethylformamide / 20 °C 5.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 6.1: 99 percent / HCl / dioxane / 20 - 45 °C 7.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1.1: 82 percent / HCl / dioxane; N,N-dimethyl-acetamide / 0.67 h / 90 °C 2.1: pentafluorophenyl trifluoroacetate; pyridine / dimethylformamide / 0.5 h / 20 °C 2.2: 94 percent / dimethylformamide / 20 - 90 °C 3.1: 59 percent / potassium iodide / N,N-dimethyl-acetamide / 50 °C 4.1: tetrazole / dimethylformamide / 20 °C 4.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 5.1: 99 percent / HCl / dioxane / 20 - 45 °C 6.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1.1: pentafluorophenyl trifluoroacetate; pyridine / dimethylformamide / 0.5 h / 20 °C 1.2: 94 percent / dimethylformamide / 20 - 90 °C 2.1: 59 percent / potassium iodide / N,N-dimethyl-acetamide / 50 °C 3.1: tetrazole / dimethylformamide / 20 °C 3.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 4.1: 99 percent / HCl / dioxane / 20 - 45 °C 5.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224
反应条件
1.1: 92 percent / NaH / N,N-dimethyl-acetamide / 60 - 110 °C 2.1: 70 percent / SOCl2; N,N-dimethylacetamide / 1 h / 85 °C 3.1: 82 percent / HCl / dioxane; N,N-dimethyl-acetamide / 0.67 h / 90 °C 4.1: pentafluorophenyl trifluoroacetate; pyridine / dimethylformamide / 0.5 h / 20 °C 4.2: 94 percent / dimethylformamide / 20 - 90 °C 5.1: 59 percent / potassium iodide / N,N-dimethyl-acetamide / 50 °C 6.1: tetrazole / dimethylformamide / 20 °C 6.2: 63 percent / aq. hydrogen peroxide / dimethylformamide / 2 h / 20 °C 7.1: 99 percent / HCl / dioxane / 20 - 45 °C 8.1: 73 percent / cyclohexene oxide / methanol / 20 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 9 p. 2213 - 2224