反应详情

3-Fluoro-4-(1-methylethoxy)benzoic acid (100 mg, 0.505 mmol) was dissolved in dichloromethane (2.5 mL). The resultant mixture was added with methoxymethylamine hydrochloride (99 mg, 1.01 mmol), WSC-HCl (106 mg, 0.555 mmol), triethylamine (422 μL, 3.03 mmol), and HOBt-H2O (34 mg, 0.252 mmol) sequentially, and stirred at room temperature overnight. The reaction solution was added with water and extracted with ethyl acetate. The organic layer was washed with 5% aqueous solution of hydrochloric acid, a saturated aqueous solution of sodium hydrogen carbonate and brine, dried using anhydrous sodium sulfate, and concentrated in vacuo. 3-Fluoro-4-(1-methylethoxy)-N-methoxy-N-methylbenzamide (117 mg, yield 96%) was obtained as a colorless oil.

1. extractionextracted with ethyl acetate
2. washThe organic layer was washed with 5% aqueous solution of hydrochloric acid
3. dry with materiala saturated aqueous solution of sodium hydrogen carbonate and brine, dried
4. concentrationconcentrated in vacuo