反应详情

温度

0 °C

N-Cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-(3-hydroxypropyl)-1H-1,2,3-triazole-4-carboxamide (3.57 g, 10 mmol) obtained in Example 113 and mesyl chloride (1.37 g, 12 mmol, 1.2 eq.) were dissolved in dichloromethane (50 ml) and triethylamine (1.21 g, 12 mmol, 1.2 eq.) was added dropwise over 10 min while stirring at 0° C. The reaction mixture was stirred at 0° C. for 1 hr. The reaction mixture was washed with 10% brine and saturated brine, dried over anhydrous sodium sulfate and concentrated. Diethyl ether was added and the precipitate was collected by filtration, washed with diethyl ether and dried to give the title compound as a white powder (4.25 g, 97.6%).

1. stirringThe reaction mixture was stirred at 0° C. for 1 hr
2. washThe reaction mixture was washed with 10% brine and saturated brine
3. dry with materialdried over anhydrous sodium sulfate
4. concentrationconcentrated
5. additionDiethyl ether was added
6. filtrationthe precipitate was collected by filtration
7. washwashed with diethyl ether
8. customdried