反应详情

温度

0 °C

N-Cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-[(phenylsulfinyl)methyl]-1H-1,2,3-triazole-4-carboxamide (107 mg, 0.24 mmol) obtained in Example 313 was dissolved in THF (2.0 ml), m-chloroperbenzoic acid (purity 65%, 64 mg, 0.24 mmol, 1.0 eq.) was added with stirring at 0° C., and the mixture was stirred for 1 hr and at room temperature for 2 hr. The reaction mixture was diluted with ethyl acetate (25 ml), washed with 5% aqueous sodium sulfite solution, 2% aqueous sodium carbonate solution and saturated brine, dried over anhydrous sodium sulfate and concentrated. Diethyl ether was added to the residue, and the precipitate was collected by filtration, washed with diethyl ether and dried to give the title compound as a white powder (111 mg, 0.24 mmol, quant.).

1. stirringthe mixture was stirred for 1 hr and at room temperature for 2 hr
2. washwashed with 5% aqueous sodium sulfite solution, 2% aqueous sodium carbonate solution and saturated brine
3. dry with materialdried over anhydrous sodium sulfate
4. concentrationconcentrated
5. additionDiethyl ether was added to the residue
6. filtrationthe precipitate was collected by filtration
7. washwashed with diethyl ether
8. customdried