反应详情

Ethyl 5-amino-1,4-dimethyl-1H-indole-2-carboxylate hydrochloride (400 mg) obtained in Reference Example 45 was suspended in DMF (4.0 mL), ethyldiisopropylamine (0.25 mL), 4-(cyclopropylmethoxy)benzoic acid (300 mg), 1-hydroxybenzotriazole monohydrate (456 mg), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (568 mg) and N,N-dimethylaminopyridine (200 mg) were successively added, and the mixture was stirred at room temperature for 22 hr. After dilution with THF and ethyl acetate, water was added. The organic layer was washed twice with water, and concentrated under reduced pressure. The residue was suspended in diisopropyl ether, and the precipitate was collected by filtration, washed with diisopropyl ether, and dried under reduced pressure to give the title compound (547 mg, yield 90%) as a white solid.

1. washThe organic layer was washed twice with water
2. concentrationconcentrated under reduced pressure
3. filtrationthe precipitate was collected by filtration
4. washwashed with diisopropyl ether
5. customdried under reduced pressure