反应 #2358521

反应方程式

CH2Cl2

1-(2-bromoethoxy)-3-fluoro-5-methylsulfonyl-benzene

azetidine

potassium carbonate

→

1-[2-(3-fluoro-5-methylsulfonyl-phenoxy)ethyl]azetidine

溶剂

acetonitrile

反应条件

后处理

1. 1
   温度The reaction mixture was cooled to room temperature
2. 2
   过滤solids was filtered off
3. 3
   其他the volatiles were evaporated
4. 4
   其他re-crystallized from methanol/diethyl ether

实验过程

1-(2-bromoethoxy)-3-fluoro-5-methylsulfonyl-benzene (0.5 g, 1.6 mmol), azetidine (0.23 ml, 3.2 mmol) and potassium carbonate (0.58 g, 4.2 mmol) was dissolved in acetonitrile (10 ml). The mixture was heated in a sealed container at 120° C. for 2 h. The reaction mixture was cooled to room temperature, CH2Cl2 (100 ml) was added, solids was filtered off and the volatiles were evaporated. The amine was converted to the fumaric acid salt and re-crystallized from methanol/diethyl ether. MS m/z (relative intensity, 70 eV) 273 (M+, 1), 94 (5), 82 (3), 71 (5), 70 (bp).

来源