反应详情

温度

80 °C

330 mg (2.17 mmol) of CsF, 81 mg (0.63 mmol) of thienylboronic acid and 36 mg (0.031 mmol) of tetrakis triphenylphosphine palladium (Pd(PPh3)4 were added to 100 mg (0.31 mmol) of 2-(4-bromophenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)acetamide) in 25 mL of DME and 2 mL of MeOH. The mixture was shaken 48 hrs at 80° C. under nitrogen. The reaction mixture is evaporated, redissolved in ethyl acetate and then washed with a saturated solution of NaHCO3. The organic layer was, after treatment with anhydrous sodium sulfate, evaporated under reduced pressure and the title compound was obtained by crystallization from acetone (48 mg, 48% yield).

1. customThe reaction mixture is evaporated
2. dissolutionredissolved in ethyl acetate
3. washwashed with a saturated solution of NaHCO3
4. customafter treatment with anhydrous sodium sulfate, evaporated under reduced pressure