反应详情

Hydroxylamine free base (50% aqueous solution, 2.0 g, 30.3 mmol) was dropwise added to diethyl maleate (4.41 g, 25.6 mmol) and stirred for 60 minutes at 40°-45° C. to give diethyl N-hydroxyaspartate. Toluene (5.02 g) and p-toluenesulfonic acid (0.05 g, 0.26 mmol) were added to the reaction mixture and refluxed for 4.5 hours. The reaction mixture was analyzed by GLC, which showed that the reaction proceeded to give 89% diethyl 2-aminomaleate (80% yield based on the external standard).