Reaktion #2358521

Reaktionsgleichung

CH2Cl2

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

azetidine

potassium carbonate

→

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

Lösungsmittel

acetonitrile

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturThe reaction mixture was cooled to room temperature
2. 2
   Filtrationsolids was filtered off
3. 3
   Sonstigethe volatiles were evaporated
4. 4
   Sonstigere-crystallized from methanol/diethyl ether

Vorschrift

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).

Quelle