反应详情

A mixture of 3(R)-phthalimido-2,3-dihydro-1,5-(5H)-benzothiazepin-4-one (10 g), ethanol (500 ml) and hydrazine hydrate (6.2 g) is refluxed for 1 hour. After ethanol is removed by evaporation under reduced pressure, water (300 ml) is added, and the mixture is extracted with ethyl acetate (400 ml). The extract is washed with 0.1 N sodium hydroxide solution (100 ml×2) and water (100 ml) successively, dried over anhydrous magnesium sulfate and concentrated in vacuo to give 3(R)-amino-2,3-dihydro-1,5(5H)-benzothiazepin-4-one (3.75 g) as colorless leaflets.

1. temperatureis refluxed for 1 hour
2. customAfter ethanol is removed by evaporation under reduced pressure, water (300 ml)
3. additionis added
4. extractionthe mixture is extracted with ethyl acetate (400 ml)
5. washThe extract is washed with 0.1 N sodium hydroxide solution (100 ml×2) and water (100 ml) successively
6. dry with materialdried over anhydrous magnesium sulfate
7. concentrationconcentrated in vacuo