反应详情

温度

0 °C

To an ice-cooled solution of N-(1-(2-hydroxyethyl)-1H-pyrazol-4-yl)-5-(m-tolyl)oxazole-4-carboxamide (2.57 g, 8.23 mmol) in DCM (70 mL), Et3N (3.44 mL, 24.69 mmol) was added. After stirring for 20 min at 0° C., p-toluenesulfonyl chloride (1.73 g, 9.05 mmol), was added dropwise, and the resulting suspension was stirred at 0° C. for 3 h, then quenched with water and extracted with DCM (2×). The combined org. layers were washed with 1 N aq. HCl-solution and brine, dried (MgSO4), filtered and concentrated in vacuo to obtain the title compound as an oil. LC-MS conditions A: tR=0.93 min, [M+H]+=467.46.

1. additionwas added
2. stirringthe resulting suspension was stirred at 0° C. for 3 h
3. customquenched with water
4. extractionextracted with DCM (2×)
5. washlayers were washed with 1 N aq. HCl-solution and brine
6. dry with materialdried (MgSO4)
7. filtrationfiltered
8. concentrationconcentrated in vacuo