4-[[2-乙氧基-5-[(4-甲基-1-哌嗪)磺酰基]苯甲酰基]氨基]-1-甲基-3-丙基-1H-吡唑-5-羧酰胺合成路线 （共 12 条）
反应条件
1: diethyl sulphate; 2-hydroxy-5-(4-methylpiperazin-1-ylsulphonyl)benzoic acid in N,N-dimethyl-formamide T=60°C; Alkylation; 2: With HOBt-6-carboxamidomethyl polystyrene; bromo-tris(1-pyrrolidinyl)phosphonium hexafluorophosphate in N,N-dimethyl-formamide Condensation; 3: 4-amino-1-methyl-3-propyl-1H-pyrazole-5-carboxamide With isocyanate resin in tetrahydrofuran Acylation;
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 10, # 17 p. 1983 - 1986
反应条件
1.1: iPr2NEt / dimethylformamide 2.1: dimethylformamide / 60 °C 2.2: polymer-supported HOBt; PyBrOP / dimethylformamide 2.3: isocyanate resin / tetrahydrofuran View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 10, # 17 p. 1983 - 1986
反应条件
1.1: iPr2NEt / dimethylformamide 2.1: dimethylformamide / 60 °C 2.2: polymer-supported HOBt; PyBrOP / dimethylformamide 2.3: isocyanate resin / tetrahydrofuran View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 10, # 17 p. 1983 - 1986
反应条件
1.1: 90 percent / MnO2 2.1: 90 percent / polymer-supported BEMP / ethanol 3.1: NH3 4.1: dimethylformamide / 60 °C 4.2: polymer-supported HOBt; PyBrOP / dimethylformamide 4.3: isocyanate resin / tetrahydrofuran View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 10, # 17 p. 1983 - 1986
反应条件
1.1: NH3 2.1: dimethylformamide / 60 °C 2.2: polymer-supported HOBt; PyBrOP / dimethylformamide 2.3: isocyanate resin / tetrahydrofuran View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 10, # 17 p. 1983 - 1986
反应条件
1: thionyl chloride; chlorosulfonic acid / 20 °C 2: sodium hydroxide / water / 2.08 h / 10 - 20 °C 3: ethyl acetate / 2.5 h / 55 °C / |Reflux 4: ethyl acetate / 70 h / 20 °C View Scheme
参考文献
Organic Process Research and Development, , vol. 4, # 1 p. 17 - 22
反应条件
1.1: nitric acid; sulfuric acid / 10 h / 50 - 55 °C / |Large scale 2.1: thionyl chloride / toluene; N,N-dimethyl-formamide / 6 h / 50 - 60 °C 2.2: 1.67 h / 20 °C 3.1: hydrogen; 5 palladium on charcoal / ethyl acetate / 4 h / 50 °C / 2585.81 Torr 4.1: ethyl acetate / 70 h / 20 °C View Scheme
参考文献
Organic Process Research and Development, , vol. 4, # 1 p. 17 - 22
反应条件
1.1: thionyl chloride / toluene; N,N-dimethyl-formamide / 6 h / 50 - 60 °C 1.2: 1.67 h / 20 °C 2.1: hydrogen; 5 palladium on charcoal / ethyl acetate / 4 h / 50 °C / 2585.81 Torr 3.1: ethyl acetate / 70 h / 20 °C View Scheme
参考文献
Organic Process Research and Development, , vol. 4, # 1 p. 17 - 22
反应条件
1: hydrogen; 5 palladium on charcoal / ethyl acetate / 4 h / 50 °C / 2585.81 Torr 2: ethyl acetate / 70 h / 20 °C View Scheme
参考文献
Organic Process Research and Development, , vol. 4, # 1 p. 17 - 22
反应条件
1: sodium hydroxide / water / 2.08 h / 10 - 20 °C 2: ethyl acetate / 2.5 h / 55 °C / |Reflux 3: ethyl acetate / 70 h / 20 °C View Scheme
参考文献
Organic Process Research and Development, , vol. 4, # 1 p. 17 - 22
