甲泼尼龙醋酸酯的醇解和水解工艺对比

Comparison between alcoholysis and hydrolysis of methylprednisolone acetate

通过HPLC监控甲泼尼龙醋酸酯醇解和水解反应过程,分别优化得出醇解和水解最佳工艺条件。对比研究结果表明,甲泼尼龙醋酸酯水解工艺优于醇解工艺。最佳水解工艺条件为:以四氢呋喃为溶剂,温度控制在5℃下并缓慢滴加碳酸钾水溶液,反应时间为3 h。此时,甲泼尼龙的收率为82. 4%,纯度为99. 78%。与醇解工艺相比,该方法具有反应过程杂质少、收率高、反应温度温和等优点,更利于大规模工业化生产。

The optimum operation conditions of alcoholysis process and hydrolysis process both for methylprednisolone acetate are respectively obtained by using HPLC as monitor.Comparative studies show that the hydrolysis process of methylprednisolone acetate is better than alcoholysis process.The best hydrolysis process conditions for methylprednisolone acetate include that tetrahydrofuran is used as solvent,the reaction temperature is controlled at5℃,the reaction lasts for 3 h and aqueous potassium carbonate solution is added slowly.The yield and purity of methylprednisolone are 82.4%and 99.78%,respectively under the best conditions.The hydrolysis process has many merits such as fewer impurities,higher yield and milder reaction temperature than alcoholysis process,and suitable for large-scale industrial production.