磷酸肌酸钠的合成

Synthesis of Phosphocreatine Disodium

通过对磷酸肌酸钠的合成研究,确定了磷酸肌酸钠的合成路线,并可以用于工业化生产。该工艺条件与其他路线比较,具有起始原料易得、反应条件温和、产品收率高、操作简便等优点。即以肌酸酐为起始原料与磷酸三乙酯混合,在超声条件下滴加三氯氧磷,缩合反应后得到肌酐磷酰氯,然后用氢氧化钠水解开环得到磷酸肌酸钠粗品,粗品用大孔树脂搅拌吸附和重结晶后得到磷酸肌酸钠精制品,结构经-1H-NMR确认,总收率65%,含量大于99.9%,产品质量符合2015版药典要求。

After researched in the synthesis of phosphocreatine disodium, the synthesis routine of phosphocreatine disodium was confirmed and can be used for industrial production. Compared with other routes, the process conditions had the advantage of initial reactants, mild reaction conditions, high yield and simple operation. With creatinine as raw material, mix with triethyl phosphate, and then added phosphorus oxychloride under the condition of ultrasound, phosphoccreatinine disodium resulted from the condensation reaction, and then cleavaged of the lactam cycle in the presence of sodroxide. The crude products stired with macroporous resin adsorption. Phosphocreatine sodium resulted from the recrystallization. Structure was confirmed by the 1H-NMR. Phosphocreatine disodium was in good yield （65%）, content was more than 99.9%. The quality of phosphocreatine disodium can meet the requirement of CP2015.