Sodium Carbonate → 3-chloro-1-(4-fluorophenyl)pyrazin-2(1H)-one

Participants

Reaction Conditions

Reaction Steps

Phosphorus oxychloride (0.94 mL, 10 mmol) was added to a solution of 3-cyclohexyloxy-1-(4-fluoro-phenyl)-1H-pyrazin-2-one (0.97 g, 3.36 mmol) in DCE (10 mL). The reaction mixture was stirred at 160° C. for 15 minutes under microwave irradiation. The reaction was poured into ice-water, then basified with a saturated solution of Na2CO3 and extracted with DCM. The organic layer was separated, dried (Na2SO4), filtered and the solvents evaporated in vacuo to yield 3-chloro-1-(4-fluoro-phenyl)-1H-pyrazin-2-one (0.71 g, 95% yield) that was used in the next step without further purification.

Provenance & Evidence