反应详情

温度

100 °C

Cyclopropyl boronic acid (1.6 g, 18.7 mmol), palladium (II) acetate (323 mg, 1.44 mmol), tricyclohexylphosphine (808 mg, 2.88 mmol) and potassium phosphate (10.7 g, 50.5 mmol) were added to a solution of 3-bromo-1-(4-(trifluoromethyl)phenylsulfonyl)-1H-pyrrole (5.11 g, 14.4 mmol) in toluene/H2O (75 mL, 19/1). The resulting suspension was evacuated and purged with nitrogen three times and then placed in an oil bath pre-heated to 100° C. The reaction was stirred for 6 h and was subsequently concentrated under vacuum. The residue was purified on a silica gel column (eluant hexane/EtOAc, 9/1, v/v) to give compound 113 (3.21 g, 10.1 mmol, 71%). MS (ESI) 316.1 (M+H).

1. customThe resulting suspension was evacuated
2. custompurged with nitrogen three times
3. customplaced in an oil bath
4. concentrationwas subsequently concentrated under vacuum
5. customThe residue was purified on a silica gel column (eluant hexane/EtOAc, 9/1