Réaction #2358521

Équation de réaction

CH2Cl2

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

azetidine

potassium carbonate

→

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

Solvants

acetonitrile

Conditions de réaction

Traitement

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

Mode opératoire

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).

Source