反应详情

(4-[(Cyclopropylamino)carbonyl]-1-{4-[(ethylamino)carbonyl]phenyl}-1H-1,2,3-triazol-5-yl)methyl methanesulfonate (204 mg, 0.501 mmol) obtained in Example 126a), potassium carbonate (69.2 mg, 0.501 mmol, 1.0 eq.) and pyrrolidine (0.084 ml, 1.00 mmol, 2.0 eq.) were suspended in acetonitrile (4.0 ml), and the mixture was stirred at room temperature for 110 min. The reaction mixture was diluted with ethyl acetate (30 ml), washed twice with 2% aqueous sodium carbonate solution and with saturated brine, dried over anhydrous sodium sulfate, and concentrated to give a colorless oil. The oil was crystallized from ethyl acetate and diethyl ether, and the precipitate was collected by filtration, washed with diethyl ether and dried to give the title compound as a white powder (160 mg, 0.418 mmol, 83.5%).

1. washwashed twice with 2% aqueous sodium carbonate solution and with saturated brine
2. dry with materialdried over anhydrous sodium sulfate
3. concentrationconcentrated
4. customto give a colorless oil
5. customThe oil was crystallized from ethyl acetate and diethyl ether
6. filtrationthe precipitate was collected by filtration
7. washwashed with diethyl ether
8. customdried