反应详情

To a solution of 1-(6-chloronaphthalene-2-sulfonyl)piperazine hydrochloride (143 mg) and triethylamine (208 mg) in dichloromethane (10 ml) was added 4-amidinobenzoylchloride hydrochloride (108 mg), and the solution was stirred at room temperature for 1 hour, to which were added DMF (10 ml) and methyl chloroformate (200 mg). The solution was stirred at 50° C. for 30 minutes and the reaction solution was concentrated . The residue was dissolved in ethyl acetate, washed with water and sodium chloride solution, dried and concentrated. The residue was purified with silica gel column chromatography (ethyl acetate/methanol=40:1) to give colorless crystals of the title compound (41 mg).

1. stirringThe solution was stirred at 50° C. for 30 minutes
2. concentrationthe reaction solution was concentrated
3. dissolutionThe residue was dissolved in ethyl acetate
4. washwashed with water and sodium chloride solution
5. customdried
6. concentrationconcentrated
7. customThe residue was purified with silica gel column chromatography (ethyl acetate/methanol=40:1)