盐酸美金刚的合成

Synthesis of memantine hydrochloride

摘要:

以1,3-二甲基金刚烷为起始原料，在N-羟基邻苯二甲酰亚胺催化下与浓硝酸硝化、在1MP氢气下以10%钯碳催化氢化、与浓盐酸成盐制得盐酸美金刚，总收率达80.54%。探讨了催化剂、浓硝酸、反应温度、反应时间对硝化反应转化率和收率的影响。以异丙醇-水为重结晶溶剂，得到纯度为99.87%的盐酸美金刚。化合物的结构经氢谱（1H-NMR）和高分辨率质谱（HR-MS）确证。

Abstract:

Memantine hydrochloride was synthesized from 1, 3-dimethyladamantane through nitration with HNO3 and N-hydroxyphthalimide, hydrogenation under 1MP hydrogen and 10% Pd-C, formation of salt with concentrated HCl. The overall yield reached 80.54%. Optimum condition of nitration was investigated, such as catalyst, quantity of HNO3, reaction time and reaction temperature. Memantine hydrochloride was recrystallized with isopropanol-water and the purity reached 99.87%. Structure of target compound was verified by 1H-NMR and HR-MS.