反应详情

温度

95 °C

A mixture of azetidine HCl salt (590 mg, 6.3 mmol), 5-bromo-2-fluoropyridine (1.11 g, 6.3 mmol), Cs2CO3 (4.1 g, 12.6 mmol) and dry DMSO (7 mL) was stirred and heated at 95° C. for 20 h. The reaction mixture was cooled and filtered. The solid was treated with H2O, extracted with CH2Cl2×3. The combined organic layers were dried, filtered to provide 1.15 grams (86%) of desired product as a light yellow solid. MS (M+H+)=213.0/215.0. 1H NMR (CDCl3) δ 8.18 (d, 1 H), 7.50 (dd, 1H), 6.18 (d, 1H), 4.03 (t, 4H), 2.40 (q, 2H).

1. temperatureThe reaction mixture was cooled
2. filtrationfiltered
3. additionThe solid was treated with H2O
4. extractionextracted with CH2Cl2×3
5. customThe combined organic layers were dried
6. filtrationfiltered