| 第 50 卷第 3 期 |  | Vol. 50 No. 3 | | 2020 年 6 月 | Jun 2020 |
|
所屬欄目：醫藥及中間體
沙曲硝唑的合成研究 |
| 李成利，劉 洋，王穎超，李博濤
（西安萬(wàn)隆制藥股份有限公司，陜西 西安 710119） |
| 摘 要：以2-巰基-1-甲基咪唑為原料，經(jīng)甲基化、硝化、氧化、縮合4步反應制得沙曲硝唑。目標化合物結構經(jīng)1H NMR、13C NMR、MS、IR確證�？疾炝朔磻獪囟�、催化劑用量、物料配比等對反應的影響。優(yōu)化條件下，合成沙曲硝唑的總收率達21.6%。優(yōu)化后的合成工藝操作簡(jiǎn)單、收率高、成本低，適合工業(yè)化生產(chǎn)。 |
| 關(guān)鍵詞：沙曲硝唑；硝基咪唑；合成 |
| 中圖分類(lèi)號：O626 文獻標識碼：A 文章編號：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 |
|
作者簡(jiǎn)介：李成利（1983-），男，甘肅鎮原人，工程師，主要從事原料藥合成研究及中試放大生產(chǎn)（E-mail：378341567@qq.com）。
|
收稿日期：2020-04-13
|
|