反应详情

To a solution of 1-[4-(piperidin-4-yl)benzoyl]-4-(6-chloronaphthalene-2-sulfonyl)piperazine hydrochloride (40 mg) and triethylamine (156 mg) in methanol (15 ml) was added ethyl acetimidate hydrochloride (46 mg), and the solution was stirred at room temperature for 15 hours. The reaction solution was concentrated. To the residue was added 1 N sodium hydroxide solution, and the solution was extracted with dichloromethane. The extract was dried and concentrated. The residue was dissolved in ethyl acetate, to which was added 4 N hydrochloric acid in ethyl acetate. The precipitate was filtered, washed with ether and dried to give a colorless solid of the title compound (42 mg).

1. concentrationThe reaction solution was concentrated
2. additionTo the residue was added 1 N sodium hydroxide solution
3. extractionthe solution was extracted with dichloromethane
4. customThe extract was dried
5. concentrationconcentrated
6. dissolutionThe residue was dissolved in ethyl acetate, to which
7. additionwas added 4 N hydrochloric acid in ethyl acetate
8. filtrationThe precipitate was filtered
9. washwashed with ether
10. customdried