反应详情

3,4-difluoro-nitrobenzene (100 g, 0.63 mol) was added dropwise to morpholine (60 g, 0.69 mol) and triethylamine (70 g, 0.69 mol) in ethyl acetate (300 mL) within 1 hour while maintaining the temperature below 50° C. The mixture is stirred at 45˜50° C. for 10 hours until the completion of the reaction. The mixture was extracted with ethyl acetate, washed with brine and dried over anhydrous magnesium sulfate, filtered, dried, to provide 138 g of yellow solid in 97% yield.

1. temperaturewhile maintaining the temperature below 50° C
2. extractionThe mixture was extracted with ethyl acetate
3. washwashed with brine
4. dry with materialdried over anhydrous magnesium sulfate
5. filtrationfiltered
6. customdried