反应详情

Add hydrogen peroxide (30% by weight, 2.39 g, 70.3 mmol) to a solution of 3-amino-3-(4-methoxyphenyl)-2-methyl-thioacrylamide (7.800 g, 35.135 mmol) in methanol (703 mL). Stir 3 h. Quench the reaction with Na2S2O3 (20% in water) and evaporate to 10 mL. Dilute with EtOAc (500 mL) and wash the organic phase with brine (3×100 mL), evaporate and crystallize from EtOAc/hexane to afford 3-(4-methoxy-phenyl)-4-methylisothiazol-5-ylamine. Yield: 88.2%. ES-MS: m/e 221.0 (m+1).

1. customQuench
2. customthe reaction with Na2S2O3 (20% in water)
3. customevaporate to 10 mL
4. additionDilute with EtOAc (500 mL)
5. washwash the organic phase with brine (3×100 mL)
6. customevaporate
7. customcrystallize from EtOAc/hexane