反应详情

To a refluxing solution of 4.3 g of (-)-cis-2-(4-methoxyphenyl)-3-hydroxy-5-[2-(N-benzyl-N-methylamino)ethyl]-8-chloro-2,3-dihydro-1,5-benzothiazepin-4(5H)-one in 50 ml of benzene, a solution of 4.55 g of benzyloxycarbonyl chloride in 10 ml of benzene is added dropwise for 15 minutes. The mixture is refluxed for one hour, and said mixture is evaporated under reduced pressure to remove solvent. 30 ml of ethanol and 50 ml of an aqueous sodium hydroxide solution are added to the residue, and the mixture is stirred at room temperature for 2 hours. Then, the mixture is diluted with water, and the aqueous mixture is extracted with chloroform. The extract is washed with water, dried and evaporated to remove solvent. 4.79 g of (-)-cis-2-(4-methoxyphenyl)-3-hydroxy-5-[2-(N-benzyloxycarbonyl-N-methylamino)ethyl]-8-chloro-2,3-dihydro-1,5-benzothiazepin-4(5H)-one are obtained.

1. temperatureThe mixture is refluxed for one hour
2. customis evaporated under reduced pressure
3. customto remove solvent
4. addition30 ml of ethanol and 50 ml of an aqueous sodium hydroxide solution are added to the residue
5. additionThen, the mixture is diluted with water
6. extractionthe aqueous mixture is extracted with chloroform
7. washThe extract is washed with water
8. customdried
9. customevaporated
10. customto remove solvent