反应详情

A mixture of 4.4 g of (+)-cis-2-(4-methoxyphenyl)-3-hydroxy-7,8-dimethyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, 2.12 g of 2-(dimethylamino)ethyl chloride hydrochloride, 4.06 g of potassium carbonate and 200 ml of acetone is refluxed for 20 hours. After the reaction is completed, insoluble materials are removed by filtration and then washed with ethanol. The filtrate and the washing are combined and then evaporated to remove solvent. The residue is dissolved in ethyl acetate, and the solution is washed with water, dried and then evaporated to remove solvent. The residue is recrystallized from a mixture of ethyl acetate and n-hexane. 4.85 g of (+)-cis-2-(4-methoxyphenyl)-3-hydroxy-5-[2-(dimethylamino)ethyl]-7,8-dimethyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one are obtained.

1. temperatureis refluxed for 20 hours
2. custominsoluble materials are removed by filtration
3. washwashed with ethanol
4. customevaporated
5. customto remove solvent
6. dissolutionThe residue is dissolved in ethyl acetate
7. washthe solution is washed with water
8. customdried
9. customevaporated
10. customto remove solvent
11. customThe residue is recrystallized from a mixture of ethyl acetate and n-hexane