تفاعل #2358521

معادلة التفاعل

CH2Cl2

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

azetidine

potassium carbonate

→

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

المذيبات

acetonitrile

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةThe reaction mixture was cooled to room temperature
2. 2
   ترشيحsolids was filtered off
3. 3
   أخرىthe volatiles were evaporated
4. 4
   أخرىre-crystallized from methanol/diethyl ether

الإجراء التجريبي

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).

المصدر