反应详情

2-Chloromethyl-N-[4-methoxy-7-(tetrahydro-pyran-4-yl)-benzothiazol-2-yl]-isonicotinamide (300 mg, 0.72 mmol) and morpholine (2.1 ml, 25 mmol) are heated to 30° C. for 30 min. The mixture is then cooled to room temperature, treated with dichloromethane (15 ml) and saturated aqueous sodium carbonate (15 ml), the phases are separated and the aqueous layer extracted twice with dichloromethane. The combined organic phases were dried over sodium sulfate and concentrated in vacuo. Flash chromatography (silica, eluent chloroform/ethyl acetate, then chloroform/methanol) afforded the title compound as white solid (60% yield). MS: m/e=469(M+H+), mp 199-201° C.

1. customthe phases are separated
2. extractionthe aqueous layer extracted twice with dichloromethane
3. dry with materialThe combined organic phases were dried over sodium sulfate
4. concentrationconcentrated in vacuo