反应详情

5.05 g of potassium carbonate are added to a mixture of 10.0 g of (+)-cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, 5.52 g of 2-(N-methyl-N-ethylamino)ethyl chloride hydrochloride and 100 ml of acetone. The mixture is refluxed under stirring overnight. After the reaction, the mixture is condensed under reduced pressure. The residue is dissolved in a mixture of ethyl acetate and water. The ethyl acetate layer is collected, dried and then evaporated to remove solvent. The residue is converted to its hydrochloride and then recrystallized from isopropanol. 12.28 g of (+)-cis-2-(4-methoxyphenyl)-3-hydroxy-5-[2-(N-methyl-N-ethylamino)ethyl]-2,3-dihydro-1,5-benzothiazepin-4(5H)-one hydrochloride are thereby obtained as colorless prisms. Yield: 87%.

1. temperatureThe mixture is refluxed
2. customAfter the reaction
3. customcondensed under reduced pressure
4. customThe ethyl acetate layer is collected
5. customdried
6. customevaporated
7. customto remove solvent
8. customrecrystallized from isopropanol