反应详情

(4-[(Cyclopropylamino)carbonyl]-1-{4-[(ethylamino)carbonyl]phenyl}-1H-1,2,3-triazol-5-yl)methyl methanesulfonate (310 mg, 0.761 mmol) obtained in Example 126a), potassium carbonate (52.6 mg, 0.380 mmol, 0.5 eq.) and sodium thiophenoxide (168 mg, 1.14 mmol, 1.5 eq.) were dissolved in ethanol (6.0 ml), and the mixture was stirred at room temperature for 2 hr. The reaction mixture was diluted with ethyl acetate (30 ml) and hexane (2 ml), washed twice with 2% aqueous sodium carbonate solution and with 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 (290 mg, 0.688 mmol, 90.4%).

1. washwashed twice with 2% aqueous sodium carbonate solution and with saturated brine
2. dry with materialdried over anhydrous sodium sulfate
3. concentrationconcentrated
4. additionDiethyl ether was added
5. filtrationthe precipitate was collected by filtration
6. washwashed with diethyl ether
7. customdried