反应详情

75 ml of methylene chloride and 3.57 g(0.01 mole) of Nalbuphine were added to a 250 ml round-bottomed flask. The flask was placed in an ice bath to keep it cool. The content was stirred then gradually 0.16 mole of triethylamine was added. With rapid stirring, another 20 ml of dichloromethane solution containing 0.011 mole of propionic anhydride was added drop by drop. Afterward, the mixture was stirred at room temperature for 1 hour. 20 ml of 10% sodium carbonate solution was added to neutralize the residual acid and remove the water soluble impurities. Sodium sulfate was used to dehydrate the solution. After drying under vacuum, a Nalbuphine propionate solid was obtained. The product was purified by column chromatography.

1. customThe flask was placed in an ice bath
2. temperaturecool
3. additionwas added drop by drop
4. stirringAfterward, the mixture was stirred at room temperature for 1 hour
5. customremove the water soluble impurities
6. customAfter drying under vacuum