反应详情

A mixture of (2R)-1-(3,5-dichlorobenzoyl)-2-(3,4-dimethylbenzyl)piperazine hydrochloride (400 mg) and 4-(4-chloro-2-butynyl)morpholine hydrochloride (223 mg) in dried acetonitrile (4.0 ml) was stirred at 50° C. in the presence of is powdered potassium carbonate (534 mg) and potassium iodide (32 mg). After 3 hours, the reaction mixture was filtered and the insoluble material on the filter was washed with acetonitrile. The filtrate and the washing were combined and then concentrated in vacuo. The resulting residue was purified by column chromatography on silica gel using a mixture of ethyl acetate and methanol (1.0:1) as eluent. The product obtained was dissolved in ethyl acetate and treated with 4N hydrogen chloride in ethyl acetate to give (2R)-1-(3,5-dichlorobenzoyl)-2-(3,4-dimethylbenzyl)-4-(4-morpholino-2-butynyl)piperazine dihydrochloride (221 mg).

1. filtrationthe reaction mixture was filtered
2. washthe insoluble material on the filter was washed with acetonitrile
3. concentrationconcentrated in vacuo
4. customThe resulting residue was purified by column chromatography on silica gel using
5. additiona mixture of ethyl acetate and methanol (1.0:1) as eluent
6. customThe product obtained