反应详情

Esomeprazole magnesium trihydrate (200 g) was dissolved in a mixture of dichloromethane (1200 ml) and methanol (1200 ml) at 25-30° C., Any undissolved material was filtered off and triethylamine (2 ml) was added to the filtrate. The clear solution thus obtained was spray dried in a mini spray dryer (Model Buchi—190) with an inlet temperature of 65-68° C. and an outlet temperature of 22-42° C. in 2 to 3 hours. The solid was further dried under vacuum at 60-65° C. for 14 to 15 hours to yield 120 g of esomeprazole magnesium of amorphous form. X-ray powder diffraction pattern showed a plain halo, which demonstrates the amorphous nature of the product. The following physical characteristics were obtained: Purity 99.77% by HPLC, Chiral purity 99.90% by HPLC, SOR 145.9°, Mg content 3.4.

1. filtrationAny undissolved material was filtered off
2. additiontriethylamine (2 ml) was added to the filtrate
3. customThe clear solution thus obtained
4. customdried in a mini spray dryer (Model Buchi—190) with an inlet temperature of 65-68° C. and an outlet temperature of 22-42° C. in 2 to 3 hours
5. customThe solid was further dried under vacuum at 60-65° C. for 14 to 15 hours