反应 #1876835

反应方程式

4-fluorophenyl methyl sulfone

2-(methylthio)ethyl amine

potassium carbonate

→

4-[2-(methylthio)ethylamino]phenyl methyl sulfone

收率 47.4%

溶剂

DMF

反应条件

后处理

1. 1
   温度Upon cooling to room temperature
2. 2
   其他the mixture was partitioned between EtOAc and brine
3. 3
   干燥dried over MgSO4
4. 4
   浓缩concentrated
5. 5
   洗涤Column chromatography, eluting with ethyl acetate/hexane

实验过程

To 8.28 g (47.52 mmol) of 4-fluorophenyl methyl sulfone dissloved in 20 mL DMF was added 5.20 g (57.03 mmol) of 2-(methylthio)ethyl amine (1.2 eq.), followed by 13.13 g (95.04 mmol, 2 eq.) potassium carbonate. The mixture was heated to 65° C. and stirred for 12 h. Upon cooling to room temperature, the mixture was partitioned between EtOAc and brine, dried over MgSO4 and concentrated. Column chromatography, eluting with ethyl acetate/hexane, provided 5.53 g of 4-[2-(methylthio)ethylamino]phenyl methyl sulfone, pure by 1H NMR.

来源