反应详情

6-Methoxy-N-methyl-N-[2-(4-morpholinyl)ethyl]-1,2-benzisoxazol-3-amine (7.0 g) was dissolved in 48% hydrobromic acid (130 ml) and heated to reflux under nitrogen for 3 hours. The reaction was cooled to room temperature, neutralized with saturated sodium carbonate (Na2CO3) extracted with ethyl acetate, dried over MgSO4 and concentrated in vacuo. Flash chromatography (silica gel) eluting with 2:1 heptane/acetone provided the product (6.0 g), m.p. 91°-92° C.

1. temperatureheated
2. temperatureto reflux under nitrogen for 3 hours
3. extractionextracted with ethyl acetate
4. dry with materialdried over MgSO4
5. concentrationconcentrated in vacuo
6. washFlash chromatography (silica gel) eluting with 2:1 heptane/acetone