反应详情

温度

50 °C

A mixture of 4-chloro-2-fluoro-6-iodoaniline (0.5 g, 1.8 mmol), vinylmethylsulfone (0.2 g, 1.8 mmol), Cs2CO3 (1.17 g, 3.6 mmol) and DMF (15 mL) was heated with stirring at 50° C. overnight. The resulting mixture was poured into water and then extracted with EA (50 mL×3). The combined organic phases were dried over Na2SO4 and then concentrated. The residue was purified by column chromatography (EtOAc:PE=1:40) to give 4-chloro-2-fluoro-6-iodo-N-[2-(methylsulfonyl)ethyl]aniline (0.42 g, yield: 61%).

1. temperaturewas heated
2. extractionextracted with EA (50 mL×3)
3. dry with materialThe combined organic phases were dried over Na2SO4
4. concentrationconcentrated
5. customThe residue was purified by column chromatography (EtOAc:PE=1:40)