反应详情

To a mixture of (±)-3-{[2-(4,5-diphenyloxazol-2-yl)-2-cyclohexen-1-yl]methyl}benzoic acid (150 mg, 0.345 mmol), glycine ethyl ester hydrochloride (63 mg, 0.449 mmol) and diisopropylethylamine (0.078 ml, 0.449 mmol) in DMF (5 ml) was added 1-hydroxybenzotriazole (70 mg, 0.518 mmol) and 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride (132 mg, 0.690 mmol). After stirring the resulting mixture at room temperature for 3 hours, the reaction mixture was diluted with EtOAc (30 ml), washed with 1N-hydrochloric acid, water, saturated sodium hydrogencarbonate solution, water and brine successively, dried over magnesium sulfate, and evaporated in vacuo. The residue was purified by silica gel column chromatography (hexane:EtOAc, 2:1 elution) to give ethyl (±)-{3-{[2-(4,5-diphenyloxazol-2-yl)-2-cyclohexen-1-yl]methyl}-benzoylamino}acetate (168.9 mg, 94%).

1. washwashed with 1N-hydrochloric acid, water, saturated sodium hydrogencarbonate solution, water and brine successively
2. dry with materialdried over magnesium sulfate
3. customevaporated in vacuo
4. customThe residue was purified by silica gel column chromatography (hexane:EtOAc, 2:1 elution)