1.1: 88 percent / TEA / DMAP / acetonitrile / 3 h 2.1: 77 percent / Et3N; Bu4NI / PdCl2(dppf) / dimethylformamide; H2O / 2 h / 50 °C 3.1: 100 percent / NaOMe / methanol / 1 h / 25 °C 4.1: 85 percent / NaBH4; NiCl2*6H2O / methanol / 6 h / 25 °C 5.1: 95 percent / NaOH 6N / tetrahydrofuran / 6 h / 25 °C 6.1: TEA / acetone / 0 °C 6.2: 95 percent / NaN3 / acetone / 0 °C 7.1: 95 percent / 0.17 h / 115 °C 8.1: 95 percent / NaOMe / methanol / 25 °C 9.1: 95 percent / KOH 6N / 1,2-dimethoxy-ethane / 12 h / reflux View Scheme

1: 3-iodo-1H-indazole With potassium tert-butylate in tetrahydrofuran T=0°C; 1.25 h; 2: methyl iodide in tetrahydrofuran T=0 - 20°C;

sodium methylate

暂无反应条件数据

1: 87 percent / potassium tert-butoxide / tetrahydrofuran / 4 h / 20 °C 2: 79 percent / sodium hydrogen carbonate / tetrakis(triphenylphosphine)palladium(0) / 1,2-dimethoxy-ethane; H2O / 3 h / Heating 3: 80 percent / phosphorus oxychloride / 0.67 h / 0 - 50 °C 4: 90 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme

4-(N,N-dimethlyamino)pyridine; triethylamine T=20°C;

4-(N,N-dimethlyamino)pyridine; triethylamine in N,N-dimethyl-formamide T=0 - 20°C; 1 h; regioselective reaction;

1: 4-(N,N-dimethlyamino)pyridine; triethylamine / 20 °C 2: tetrakis(triphenylphosphine) palladium(0); sodium carbonate / 1,4-dioxane; water / 1 h / 120 °C / |Microwave irradiation View Scheme

potassium hydroxide; tetrabutylammomium bromide in dichloromethane T=0 - 20°C; 3 h;

in tetrahydrofuran