Acetyl chloride → 1-(Pyrrolo[1,2-a]pyrazin-8-yl)ethanone

Participants

Reaction Steps

20 g of pyrrolo[1,2-a]pyrazine prepared in Preparation Example 1 was dissolved in 100 ml of dichloroethane; and 30 g of aluminium trichloride and 12 g of acetylchloride were added thereto . The mixture was reacted at 60° C. for 4 hours, cooled to room temperature and then poured into 300 ml of ice-water. The mixture was adjusted to pH 10 with sodium hydroxide, extracted with 500 ml of ethyl acetate and concentrated. The residue was chromatographed over silica gel to obtain 4.5 g of 6-acetylpyrrolo[1,2-a]pyrazine and 4.0 g of 8-acetylpyrrolo-[1,2-a]pyrazine.

Provenance & Evidence