反应详情

Add boron tribromide (0.227 g, 0.909 mmol) to a solution of 3-(4-methoxy-phenyl)-4-methylisothiazol-5-ylamine (0.100 g, 0.455 mmol) in dichloromethane (5 mL) at −20° C. Stir and allow to warm to room temperature. Stir 4 h and quench with 1 N HCl. Extract with EtOAc (2 times 50 mL). Dry (MgSO4) and evaporate. The product is used for the next step without further purification. Yield: 106.8% ES-MS: m/e 207.0 (m+1).

1. stirringStir 4 h
2. customquench with 1 N HCl
3. extractionExtract with EtOAc (2 times 50 mL)
4. dry with materialDry (MgSO4)
5. customevaporate
6. customThe product is used for the next step without further purification