反应详情

Dissolve [2-(3′-chloro-2,3,5,6-tetrahydro-[1,2′]bipyrazinyl-4-yl)-ethyl]-methyl-amine hydrochloride salt (0.5 g, 1.29 mmol) in dichloromethane (10 ml) and cool in an ice-bath. Add triethylamine (0.90 ml, 6.44 mmol) and then 1,3-dimethylpyrazole-4-sulfonyl chloride (250 mg, 1.29 mmol). Remove the ice-bath and allow to warm to ambient temperature and allow to stir for 2 hr. Wash the organic phase with aqueous sodium bicarbonate, brine and water. Dry over sodium sulfate and concentrate. Purify by chromatography, eluting with 1:2 hexanes:acetone to afford the title preparation (535 mg, 100% yield) as a white foam. MS ES: m/z=414 [M+H]+.

1. temperaturecool in an ice-bath
2. customRemove the ice-bath
3. washWash the organic phase with aqueous sodium bicarbonate, brine and water
4. dry with materialDry over sodium sulfate
5. concentrationconcentrate
6. customPurify by chromatography
7. washeluting with 1:2 hexanes
8. customacetone to afford the title
9. custompreparation (535 mg, 100% yield) as a white foam