反应详情

温度

45 °C

A mixture of 2-chloromethyl-3,5-dimethoxy-pyrazine (115 mg, 0.61 mmol), 2-fluoro-6-(1H-imidazol-2-yl)-pyridine (98 mg, 0.60 mmol) and K2CO3 (250 mg, 1.81 mmol) in DMF (7 mL) is stirred at 45° C. for 16 hours. On cooling, the reaction is quenched with saturated NH4Cl (3 mL) and extracted with DCM (3×15 mL). The combined organic layers are dried and solvent removed. PTLC (silica gel) separation (10% MeOH in DCM) gives 123 mg of 2-[2-(6-fluoro-pyridin-2-yl)-imidazol-1-ylmethyl]-3,5-dimethoxy-pyrazine as an oil. LRMS calcd 315.30, found 316.20 (MH+). D. 3,5-Dimethoxy-2-(2-thiazol-2-yl-imidazol-1-ylmethyl)-pyrazinel (Compound 5)

1. temperatureOn cooling
2. customthe reaction is quenched with saturated NH4Cl (3 mL)
3. extractionextracted with DCM (3×15 mL)
4. customThe combined organic layers are dried
5. customsolvent removed
6. customPTLC (silica gel) separation (10% MeOH in DCM)