反应详情

温度

25 °C

Into a 25-mL round-bottom flask, was placed 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-2-(trifluoromethyl)benzoic acid (70 mg, 0.14 mmol, 1.00 equiv), N,N-dimethylformamide (3 mL), HATU (105 mg, 0.28 mmol, 2.00 equiv), DIEA (36 mg, 0.28 mmol, 1.96 equiv), piperazine-2,6-dione (32 mg, 0.28 mmol, 1.99 equiv). The resulting solution was stirred for 1 h at 25° C. The reaction was then quenched by the addition of 10 ml of water. The resulting solution was extracted with 2×10 mL of ethyl acetate and the organic layers combined. The resulting mixture was washed with 3×20 mL of brine. The resulting mixture was concentrated under vacuum. The residue was applied onto a TLC plate with ethyl acetate/petroleum ether (1/1). This resulted in 70 mg (76%) of 4-[(4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-2-(trifluoromethyl)phenyl)carbonyl]piperazine-2,6-dione as colorless oil.

1. customInto a 25-mL round-bottom flask, was placed
2. customThe reaction was then quenched by the addition of 10 ml of water
3. extractionThe resulting solution was extracted with 2×10 mL of ethyl acetate
4. washThe resulting mixture was washed with 3×20 mL of brine
5. concentrationThe resulting mixture was concentrated under vacuum
6. customThis resulted in 70 mg (76%) of 4-[(4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-2-(trifluoromethyl)phenyl)carbonyl]piperazine-2,6-dione as colorless oil