反应详情

Rosiglitazone maleate was prepared according to the disclosure of WO 94/05659, in which 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione (470 gms) and maleic acid (137 gms) were dissolved in ethanol (4 ltrs) at boiling. The hot solution was filtered via diatomaceous earth and was then allowed to cool slowly with gentle agitation. After leaving in a refrigerator at 0-5° C. for several hours, the maleate salt was filtered off, washed with ethanol and dried in vacuum at 50° C. to give 446 gms of rosiglitazone maleate as provided by WO 94/05659. The product was characterized as Form-B by XRD & IR, as can be seen by reference to FIGS. 3 and 4 respectively.

1. customRosiglitazone maleate was prepared
2. filtrationThe hot solution was filtered via diatomaceous earth
3. temperatureto cool slowly with gentle agitation
4. customAfter leaving in a refrigerator at 0-5° C. for several hours
5. filtrationthe maleate salt was filtered off
6. washwashed with ethanol
7. customdried in vacuum at 50° C.