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盐酸美金刚的合成
引用本文:王玉斌,陆鹏,马博,赵大敏,佘金雄. 盐酸美金刚的合成[J]. 精细化工, 2012, 29(8): 800-802
作者姓名:王玉斌  陆鹏  马博  赵大敏  佘金雄
作者单位:1. 南京工业大学药学院,江苏南京210009;南京中美肿瘤研究中心,江苏南京210009
2. 南京中美肿瘤研究中心,江苏南京,210009
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1 MPa氢气下以质量分数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%。探讨了催化剂用量、浓硝酸用量、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,得到质量分数为99.87%的盐酸美金刚。化合物的结构经氢谱(1HNMR)和高分辨率质谱(HR-MS)确证。

关 键 词:盐酸美金刚  硝化  氢化  医药与日化原料
收稿时间:2012-03-21
修稿时间:2012-04-19

Synthesis of memantine hydrochloride
WANG Yu-bin,LU Peng,MA Bo,ZHAO Da-min and SHE Jin-xiong. Synthesis of memantine hydrochloride[J]. Fine Chemicals, 2012, 29(8): 800-802
Authors:WANG Yu-bin  LU Peng  MA Bo  ZHAO Da-min  SHE Jin-xiong
Affiliation:Nanjing University of Technology,Nanjing University of Technology,Nanjing University of Technology,Nanjing University of Technology,Nanjing University of Technology
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.
Keywords:memantine hydrochloride   nitration   hydrogenation
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