Phosphorus oxychloride → HCID 76849760, compound

Participants

Reaction Conditions

Reaction Steps

To N-((3-chloropyrazin-2-yl)methyl)-4-methylpiperazine-1-carboxamide (485 mg) in acetonitrile (3 mL) under a N2 flow was added phosphorus oxychloride (878 μl) and heated at 60° C. (bath temperature) for five hours and at 80° C. for one hour. Then the reaction mixture was concentrated in vacuo. Toluene was added and the mixture was concentrated in vacuo. Residue was taken up with acetonitrile, 7N ammonia in methanol was added with cooling and the suspension was stirred for 16 hours, then filtered and the filtrate concentrated in vacuo. Dichloromethane was added to the residue, again filtered and the filtrate concentrated in vacuo to give 8-chloro-3-(4-methylpiperazin-1-yl)imidazo[1,5-a]pyrazine (400 mg).

Provenance & Evidence