反应详情

To a solution of 4-methoxy-3-[4-(2,2,2-trifluoro-acetyl)-piperazin-1-yl]-benzenesulfonyl chloride (0.19 g; 0.5 mmol) in THF (0.5 mL) at 0° C. under argon atmosphere was added dropwise a solution of 1-naphthylmagnesium bromide in THF (0.5M, 2 mL; 1 mmol). After stirring at this temperature for 1 h, a saturated solution of ammonium chloride was added and the mixture was extracted into ethyl acetate (20 mL). The organic phase was dried (Na2SO4) and concentrated in vacuo and the residue was purified by column chromatography on silica gel (eluting with hexane-ethyl acetate (7:3, v/v) to give 2,2,2-trifluoro-1-{4-[2-methoxy-5-(naphthalene-1-sulfonyl)-phenyl]-piperazin-1-yl}-ethanone (1) as a white solid (0.110 g; 47%), MS, MH+ 479.

1. extractionthe mixture was extracted into ethyl acetate (20 mL)
2. dry with materialThe organic phase was dried (Na2SO4)
3. concentrationconcentrated in vacuo
4. customthe residue was purified by column chromatography on silica gel (
5. washeluting with hexane-ethyl acetate (7:3