第 50 卷第 3 期 Vol. 50 No. 3 2020 年 6 月 Jun 2020

所属栏目：医药及中间体 沙曲硝唑的合成研究

李成利，刘 洋，王颖超，李博涛 （西安万隆制药股份有限公司，陕西 西安 710119）

摘　要：以2-巯基-1-甲基咪唑为原料，经甲基化、硝化、氧化、缩合4步反应制得沙曲硝唑。目标化合物结构经1H NMR、13C NMR、MS、IR确证。考察了反应温度、催化剂用量、物料配比等对反应的影响。优化条件下，合成沙曲硝唑的总收率达21.6%。优化后的合成工艺操作简单、收率高、成本低，适合工业化生产。

关键词：沙曲硝唑；硝基咪唑；合成

中图分类号：O626　　文献标识码：A　　文章编号：1009-9212（2020）03-0036-03

Synthesis of Satranidazole

LI Cheng-li, LIU Yang, WANG Ying-chao, LI Bo-tao (Xi'an WanLong Pharmaceutical Co.,Ltd., Xi'an 710119, China)

Abstract：1-Methanesulfonyl-3-(1-methyl-5-nitroimidazol-2-yl)-2-imidazolidinone was obtained from 2-mercapto-1-methylimidazole by a four-steps reaction process including methylation, nitration, oxidation, and condensation. The structure of the product was confirmed using 1H NMR, 13C NMR, MS, and IR. The effects of factors including reaction temperature, mass of the catalyst, and molar ratio of raw materials on the reaction were investigated. The results of experiment showed that satranidazole was obtained with a yield of 21.6% under the optimum conditions. The producing process is easy to control with high yield and low cost, and it is suitable for industrial production.

Key words：satranidazole; nitroimidazole; synthesis

作者简介：李成利（1983-），男，甘肃镇原人，工程师，主要从事原料药合成研究及中试放大生产（E-mail：378341567@qq.com）。

收稿日期：2020-04-13