反应详情

温度

90 °C

N-(6-Chloro-5-cyanopyridin-3-yl)-5-methyl-1-[5-(trifluoromethyl)pyridin-2-yl]-1H-pyrazole-4-carboxamide (200 mg), 4-[4-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)cyclohex-3-en-1-yl]morpholine (159 mg) described in Reference Example 166 and tetrakis(triphenylphosphine)palladium (57 mg) were dissolved in a mixture of tetrahydrofuran (1 ml) and 1M aqueous solution of sodium carbonate (0.54 ml), and stirred at 90° C. After completion of the reaction, the reaction solution was left stand, filtered through Celite, washed with chloroform and the filtrate was concentrated. Water was added to the resulting residue and the precipitate was filtered. The obtained solid was refluxed in ethanol, the resulting solution was left stand, the precipitated solid was collected by filtration and dried in vacuo to give the titled compound (143 mg) as a pale yellow solid.

1. customAfter completion of the reaction
2. waitthe reaction solution was left stand
3. filtrationfiltered through Celite
4. washwashed with chloroform
5. concentrationthe filtrate was concentrated
6. additionWater was added to the resulting residue
7. filtrationthe precipitate was filtered
8. temperatureThe obtained solid was refluxed in ethanol
9. waitthe resulting solution was left stand
10. filtrationthe precipitated solid was collected by filtration
11. customdried in vacuo