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), prepared as in Example 1 Step 2, in THF (0.5 ml) at 0° C. under argon atmosphere was added dropwise a solution of 4-methoxyphenylmagnesium bromide in THF (0.5M, 2 ml; 1 mmol). After stirring at this temperature for 1 h. A solution of 6N NaOH (0.5 ml) was added and the reaction mixture was stirred at ambient temperature for 20 h. Water was added (10 ml) and the mixture was extracted into ethyl acetate (20 ml). The organic phase was dried (Na2SO4) and concentrated in vacuo to give 1-[5-(4-methoxy-benzenesulfonyl)2-methoxy-phenyl]piperazine as a white solid (0.65 g, 36%), MS, MH+ 363.

1. stirringthe reaction mixture was stirred at ambient temperature for 20 h
2. extractionthe mixture was extracted into ethyl acetate (20 ml)
3. dry with materialThe organic phase was dried (Na2SO4)
4. concentrationconcentrated in vacuo