Dimethylformamide → 6-(5-chloro-2-pyridyl)-5H-pyrrolo[3,4-b]pyrazine-5,7(6H)-dione

Participants

Reaction Conditions

Reaction Steps

3-(5-Chloropyridin-2-yl)-carbamoylpyrazine-2-carboxylic acid (100 g) was suspended in 500 ml dichloromethane. The suspension was refluxed azeotropically for 60 min. The mixture was cooled to 25-30° C. and dimethyl formamide (2.6 gm) was added followed by addition of thionyl chloride (72 g) in 45-60 min at 25-30° C. The resulting mixture was refluxed till completion of reaction. The reaction mixture was concentrated to dryness at atmospheric pressure. Cooled the solid to 20-25° C. and 500 ml chilled water was added Cooled the slurry to 20-25° C. and stirred for 30 min. Slurry was filtered and washed with 200 ml water. The solid was dried at 60-70° C. to obtain 88 g of title compound.

Provenance & Evidence