第 46 卷第 1 期Vol. 46 No. 1
2016 年 2 月Feb 2016

所属栏目:医药及中间体

N-甲基硝酰胺的合成
高 勋,鲁萌萌,周启璠,陈国良* (沈阳药科大学 基于靶点的药物设计与研究教育部重点实验室,辽宁 沈阳 110016)
摘 要:以对甲苯磺酰氯为起始原料,经酰胺化、硝化、氨解3步反应,合成了目标化合物N-甲基硝酰胺,对各步反应进行了考察与优化,优化条件下,目标化合物的总收率达83.3%,其结构经1H NMR和熔点确证。该合成工艺操作简单、条件温和、试剂价廉易得,具有工业化前景。
关键词:N-甲基硝酰胺;氨解;合成
中图分类号:TQ252.3  文献标识码:A  文章编号:1009-9212(2016)01-0061-03
Synthesis of N-Methylnitramine
GAO Xun, LU Meng-meng, ZHOU Qi-fan, CHEN Guo-liang* (Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China)
Abstract:The target compound N-methylnitramine was synthesized through three steps using 4-methylbenzene-sulfonylchloride as starting material. Each reaction was investigated and optimized to get an optimum condition, the yield of the target compound was up to 83.3% and the product was characterized by 1H NMR and melting Point. This process was suitable for industrial production due to the simple procedures, mild reaction conditions and lower cost.
Key words:N-methylnitramine; ammonolysis; synthesis
作者简介:高 勋(1994-),男,湖南宁乡人,硕士研究生,主要从事药物合成及工艺研究(E-mail:gaoxuno221@163.com)。
联 系 人: 陈国良,教授,博士生导师,主要从事抗癌药物的研究(E-mail:guoliang222@gmail.com)。
收稿日期: 2015-12-2