Rosiglitazone → Rosiglitazone Maleate

関与物質

反応条件

反応手順

5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione (rosiglitazone free base, 50 gms, 0.140 mol) was charged in 100 ml methanol and a solution of maleic acid (18.7 gms, 0.16 mol) in methanol (50 ml) was added under stirring and was further heated to 45-50° C. to obtain a clear solution. This solution was filtered (hot) through celite and ethyl acetate (500 ml) was added slowly to this clear filtrate under stirring at 25-30° C., and further stirred for 1 hour at 30° C., then chilled to 5-10° C. and stirred at the same temperature for 1 hour. The solid obtained was filtered under argon atmosphere and washed with 50 ml ethyl acetate. This solid was dried under vacuum at 50-55° C. to get rosiglitazone maleate Form A (60 gms) in 90% yield.

情報源と証拠