反应详情

To a suspension of (R)-1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethanamine 2HCl salt (1.1 g, 3.8 mmol) and (E)-3-(1-(tert-butoxycarbonyl)-1H-indol-3-yDacrylic acid (1.0 g, 3.5 mmol) in dichloromethane (8 mL) were added triethylamine (1.8 g, 17 mmol), EDC (800 mg, 4.2 mmol) and HOBT (270 mg, 1.7 mmol) respectively. The reaction mixture was stirred at room temperature for 6 hours. Sat. sodium bicarbonate 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 900 mg (53% yield) of the title as a yellow solid;

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 900 mg (53% yield) of the title as a yellow solid