反应详情

温度

110 °C

To a 350 mL sealed flask reactor was added methyl 4-(4-bromo-1-methyl-1H-pyrazol-5-yl)-5-methyl-2-thiophenecarboxylate (2.57 g, 8.15 mmol), trimethylboroxine (2.27 ml, 16.31 mmol), K2CO3 (3.47 g, 25.1 mmol) and Pd(dppf)Cl2 (426 mg, 0.83 mmol) in N,N-Dimethylformamide (DMF) (41 ml). The reaction was heated at 110° C. for 1 hour. The mixture was partitioned between CHCl3/H2O, organic layer separated and dried with Na2SO4. The resulting material was adsorbed onto silica and purified via column chromatography (0-15% EtOAc/Hexane) affording the title compound (1.3 g, 4.76 mmol, 58%): LC-MS (ES) m/z=251 (M+H)+.

1. customTo a 350 mL sealed flask reactor
2. customThe mixture was partitioned between CHCl3/H2O, organic layer
3. customseparated
4. dry with materialdried with Na2SO4
5. custompurified via column chromatography (0-15% EtOAc/Hexane)