反应详情

To a suspension of (R)-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethanamine 2HCl salt (173 mg, 0.79 mmol) and 2-(4-bromophenoxy)acetic acid (200 mg, 0.87 mmol) in dichloromethane (5 mL) were added triethylamine (400 mg, 3.9 mmol), EDC (180 mg, 0.94 mmol) and HOBT (60 mg, 0.39 mmol) respectively. The reaction mixture was stirred at room temperature for 18 hours. Sat. ammonia hydrochloride aqueous solution was added to the mixture. The organic layer was extracted with ethyl acetate, washed with brine, and dried over sodium sulfate. After the filtration to separate solvent and sodium sulfate, the solvent was removed under reduced pressure to give the residue, which was applied to a silica gel chromatography column and eluted with a hexane/ethylacetate=2/1 (v/v) to furnish 276 mg (81% yield) of the title as a colorless oil;

1. extractionThe organic layer was extracted with ethyl acetate
2. washwashed with brine
3. dry with materialdried over sodium sulfate
4. filtrationAfter the filtration
5. customto separate solvent and sodium sulfate
6. customthe solvent was removed under reduced pressure
7. customto give the residue, which
8. washeluted with a hexane/ethylacetate=2/1 (v/v)
9. customto furnish 276 mg (81% yield) of the title as a colorless oil