Diisopropylethylamine → 4-([4-[5-(3,5-Dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-2-(trifluoromethyl)phenyl]carbonyl)piperazine-2,6-dione

関与物質

反応条件

反応手順

Into a 50-mL round-bottom flask, was placed a solution of 4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-2-(trifluoromethyl)benzoic acid (300 mg, 0.64 mmol, 1.00 equiv) in N,N-dimethylformamide (2 mL), HATU (483 mg, 1.27 mmol, 2.00 equiv), DIEA (164 mg, 1.27 mmol, 2.00 equiv), piperazine-2,6-dione (145 mg, 1.27 mmol, 2.00 equiv). The resulting solution was stirred for 3 h at 20° C. The resulting solution was diluted with 50 mL of brine. The resulting solution was extracted with 3×50 mL of ethyl acetate and the organic layers combined. The mixture was dried over sodium sulfate and concentrated under vacuum. The residue was applied onto a silica gel column with PE/EA (10:1). This resulted in 330 mg (91%) of 4-([4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-2-(trifluoromethyl)phenyl]carbonyl)piperazine-2,6-dione as a white solid.

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