反应详情

温度

45 °C

A mixture of 3-chloro-2-chloromethyl-5-methoxy-pyrazine (350 mg, 1.81 mmol), 2-fluoro-6-(1H-imidazol-2-yl)-pyridine (266 mg, 1.63 mmol) and K2CO3 (750 mg, 5.43 mmol) in DMF (10 mL) is stirred at 45° C. for 16 hours. On cooling, the reaction is quenched with saturated NH4Cl (3 mL) and extracted with DCM (3×20 mL). The combined organic layers are dried and solvent removed. PTLC (silica gel) separation (10% MeOH in DCM) gives 370 mg of 3-chloro-2-[2-(6-fluoro-pyridin-2-yl)-imidazol-1-ylmethyl]-5-methoxy-pyrazine as an oil. 1H NMR (CDCl3) 8.08–8.14 (m, 1H), 7.98(s, 1H), 7.81 (dd, 1H), 7.20 (s, 1H), 7.07 (s, 1H), 6.80 (dd, 1H), 6.02 (s, 2H), 3.98 (s, 3H) F. Synthesis of 2-[2-(6-Fluoro-pyridin-2-yl)-imidazol-1-ylmethyl]-5-methoxy-3-pyridin-2-yl-pyrazine (Compound 7)

1. temperatureOn cooling
2. customthe reaction is quenched with saturated NH4Cl (3 mL)
3. extractionextracted with DCM (3×20 mL)
4. customThe combined organic layers are dried
5. customsolvent removed
6. customPTLC (silica gel) separation (10% MeOH in DCM)