反応 #2358521

反応方程式

CH2Cl2

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

azetidine

potassium carbonate

→

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

溶媒

acetonitrile

反応条件

後処理

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

実験手順

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).

出典