反应详情

To a solution of 3-(3,4,5-trimethoxyphenyl)-2-(4-fluorophenyl)acrylic acid (0.6 g, 18 mmol) in DMF (5 mL) was added ethyl-4-aminomethylbenzoate.HCl (0.375 g, 21.6 mmol), EDCI (0.69 g, 36 mmol) and HOBt (0.24 g, 18 mmol). TEA (0.75 mL, 36 mmol) was added dropwise with constant stirring to the above reaction mixture and stirred overnight at room temperature. Subsequently the reaction mixture was evaporated to dryness, the residue was dissolved in ethyl acetate and washed successively with 1N HCl (3×50 mL), saturated NaHCO3 (3×50 mL) and brine solution (3×50 mL). The organic layer was dried over Na2SO4 and concentrated to give the pure compound (0.4 g, 50% yield).

1. stirringstirred overnight at room temperature
2. customSubsequently the reaction mixture was evaporated to dryness
3. dissolutionthe residue was dissolved in ethyl acetate
4. washwashed successively with 1N HCl (3×50 mL), saturated NaHCO3 (3×50 mL) and brine solution (3×50 mL)
5. dry with materialThe organic layer was dried over Na2SO4
6. concentrationconcentrated