反应详情

To a flask with E4 (310 mg, 0.77 mmol) was added 2-(4-fluoro-3-(trifluoromethyl)phenyl)acetic acid (187 mg, 0.84 mmol), EDC (440 g, 2.3 mmol), HOBt (52 mg, 0.38 mmol), followed by 14 mL of anhydrous DMF and N-methyl morpholine (0.25 mL, 2.3 mmol). The reaction was stirred at room temperature overnight and worked up with ethyl acetate and water. Column chromatography with gradient ethyl acetate/dichloromethane (3:1 to 2:1 to 1:1) gave 460 mg E5 as an yellow foamy solid.