反应详情

温度

0 °C

To a mixture of (3R,4S ,5S ,6S)-5-(5-isopropyl-2-methoxybenzylamino)-6-diphenylmethyl-1-azabicyclo[2.2.2]octane-3-carboxylic acid dihydrochloride (300 mg, 0.5 mmol), alaninamide hydrobromide (100 mg, 0.6 mmol) and triethylamine (70 mg, 0.7 mmol) in DMF (2 ml) was added 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (160 mg, 0.8 mmol) at 0° C. The mixture was stirred at 0° C. for 30 minutes, then at room temperature for 14 hours. Water and NaHCO3 were added and the mixture was extracted with CH2Cl2. The combined extracts were dried, concentrated and purified by a column chromatography on silica-gel (CH2Cl2 /methanol=10:1) to give a title compound (220 mg, 0.39 mmol, 77%).

1. waitat room temperature for 14 hours
2. extractionthe mixture was extracted with CH2Cl2
3. customThe combined extracts were dried
4. concentrationconcentrated
5. custompurified by a column chromatography on silica-gel (CH2Cl2 /methanol=10:1)