反应详情

To the solution of thietan-3-amine hydrobromide (40 mg, 0.23 mmol) in 1,2-dichloromethane was added triethylamine (60 mg, 0.59 mmol) at 0° C. After that 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (54 mg, 0.23 mmol), 1-hydroxybenzotriazole monohydrate (32 mg, 0.23 mmol), and 4-[3-(3,4,5-trichlorophenyl)-3-(trifluoromethyl)-3,4-dihydro-2H-pyrrol-5-yl]-2-(trifluoromethyl)benzoic acid (100 mg, 0.19 mmol) were added to the solution at 0° C. Then the reaction mixture was stirred overnight at room temperature and diluted with t-butylmethylether, and washed with water, and dried over magnesium sulfate anhydrous. After evaporation, the residue was purified with silicagel column chromatography to give 75 mg of N-(thietan-3-yl)-4-[3-(3,4,5-trichlorophenyl)-3-(trifluoromethyl)-3,4-dihydro-2H-pyrrol-5-yl]-2-(trifluoromethyl)benzamide.

1. washwashed with water
2. dry with materialdried over magnesium sulfate anhydrous
3. customAfter evaporation
4. customthe residue was purified with silicagel column chromatography