反应详情

温度

55 °C

4-[(Chloroacetyl-methyl-amino)-methyl]-N-(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-benzamide (100 mg, 205 mmol) are dissolved in N-(2-methoxyethyl)-methylamine (1.8 ml, 21 mmol) and the mixture stirred for 2 h at 55° C. Saturated aqueous sodium hydrogen carbonate is added (50 ml) and dichloromethane (50 ml) are added, the phases are separated and the aqueous phase extracted twice with 50 ml dichloromethane. The combined organic layers are dried with magnesium sulfate and evaporated. Flash chromatography (silica, dichloromethane containing 5% methanol) afforded the title compound as white crystals (74% yield), mp 171-173° C. MS: m/e=542 (M+H+).

1. additionare added
2. customthe phases are separated
3. extractionthe aqueous phase extracted twice with 50 ml dichloromethane
4. dry with materialThe combined organic layers are dried with magnesium sulfate
5. customevaporated