反应详情

温度

80 °C

To a solution of 3.29 g (5.23 mmol) 2-(3-chloro-pyridin-2-yl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [2-(bicyclopropyl-1 -ylcarbamoyl)-4-iodo-6-methyl-phenyl]-amide in 50 ml tetrahydrofuran is added 1.19 g (6.25 mmol) Cul, 0.30 g tetrakis(triphenylphosphine) palladium and 2.78 g (31.0 mmol) CuCN. The mixture is heated 1 h at 80° C. and turns dark green. After cooling down, the mixture is filtered on Hyflo and evaporated. The residue is dissolved in 15 ml DMF and poured into 100 ml water containing 5 g NaHCO3. After 30 min stirring, the crystals are filtered, washed with water and a mixture of hexane/acetone (1:3) to afford 2.8 g of the title compound.

1. temperatureAfter cooling down
2. filtrationthe mixture is filtered on Hyflo
3. customevaporated
4. dissolutionThe residue is dissolved in 15 ml DMF
5. additionpoured into 100 ml water containing 5 g NaHCO3
6. filtrationthe crystals are filtered
7. washwashed with water
8. additiona mixture of hexane/acetone (1:3)