反应详情

温度

55 °C

(5-{2-[(N-Cyclopropanecarbonyl-N-ethyl-amino)-methyl]-4-trifluoromethyl-phenyl}-6-hydroxy-pyridin-3-yl)-acetic acid ethyl ester (0.175 g, 0.39 mmol), 2,2,2-trifluoroethyl tosylate (0.151 g, 0.58 mmol), and potassium carbonate (0.070 g, 0.51 mmol) were combined in DMF (1.8 mL) and stirred at 55° C. overnight. Additional 2,2,2-trifluoroethyl tosylate and potassium carbonate were added, and the reaction was stirred at 75° C. overnight. After cooling, the crude material was used directly in the hydrolysis step. The ester was hydrolyzed to the acid as described in Example 3, Step 7. The acid was purified by preparative HPLC.

1. stirringthe reaction was stirred at 75° C. overnight
2. temperatureAfter cooling
3. customThe acid was purified by preparative HPLC