反应详情

A mixture of 3-chloropropane-1-sulfonic acid [2-(4-cyclopropylpiperazin-1-yl)benzothiazol-6-ylmethyl]amide (300 mg, 0.70 mmol) and potassium hydroxide (396 mg, 7.0 mmol) in EtOH (5 mL) was heated at reflux for 1 h. The volatiles were evaporated and the residue was extracted with CH2Cl2, washed with brine and concentrated in vacuo. The crude residue was purified by column chromatography on silica gel (elute: 5% CH2Cl2 in methanol) to give 2-(4-cyclopropylpiperazin-1-yl)-6-(1,1-dioxo-1λ6-isothiazolidin-2-ylmethyl)benzothiazole 193 mg (49%).

1. temperaturewas heated
2. temperatureat reflux for 1 h
3. customThe volatiles were evaporated
4. extractionthe residue was extracted with CH2Cl2
5. washwashed with brine
6. concentrationconcentrated in vacuo
7. customThe crude residue was purified by column chromatography on silica gel (elute: 5% CH2Cl2 in methanol)