反应详情

温度

80 °C

To a solution of 2-benzoimidazol-1-yl-1-(3-bromophenyl)ethanone (42.7 mg, 0.136 mmol; see step (a)) in toluene (7 mL) and ethanol (1 mL) was added 5-isobutyl-2-(N-tert-butylaminosulfonyl)thiophene-3-boronic acid (73.5 mg, 0.230 mmol; see Example 1(c)), Pd(PPh3)4 (9.4 mg, 8.1 μmol) and Na2CO3 (271 μL, 0.542 mmol, 2.0 M aq), and the reaction mixture was stirred for 3 h at 80° C. The reaction mixture was diluted with water (10 mL) and extracted with EtOAc. The combined organic phase was dried (over anhydrous MgSO4), concentrated in vacuo, and the residue was purified by flash chromatography using MeOH:CH2Cl2 (5:95) as eluent to give the sub-title compound as a colourless syrup in 90% yield (62 mg, 0.122 mmol).

1. extractionextracted with EtOAc
2. dry with materialThe combined organic phase was dried (over anhydrous MgSO4)
3. concentrationconcentrated in vacuo
4. customthe residue was purified by flash chromatography