4-氯-2-(N-甲基-N-苯基胺磺酰基）苯甲酸甲酯的合成  

Synthesis of Methyl 4-chloro-2-(N-methyl-N-phenylsulfamoyl) benzoate

作　　者：张恩乾 王俊峰 周英雷 夏春年[1,2] ZHANG En-qian;WANG Jun-feng;ZHOU Ying-lei;XIA Chun-nian(College of Pharmaceutical Science,Zhejiang University of Technology,Hangzhou 310014,China;Zhejiang Multinpharma Co.,Ltd.,Hangzhou 310014,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014 [2]浙江叠智医药科技有限公司,浙江杭州310014

出　　处：《精细化工中间体》2019年第5期33-36,共4页Fine Chemical Intermediates

摘　　要：以2-氨基-4-氯苯甲酸为原料,经重氮化、酯化、氧化缩合共3步反应,得到4-氯-2-(N-甲基-N-苯基胺磺酰基)苯甲酸甲酯(1)。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,以62.7%总收率合成了化合物1。优化合成工艺操作简单,收率高,成本低,适合工业化生产。化合物1的结构经1H NMR、13C NMR、 MS、 IR、熔点等确证。Methyl 4-chloro-2-(N-methyl-N-phenylsulfamoyl)benzoate(1) was obtained from 2-amino-4-chlorobenzoic acid by three steps which contain diazotization,esterification and oxidation condensation. And the effects of reaction temperature,mass of the catalyst,molar ratio of raw materials on the reation were investigated. The results of experiment showed that compound 1 was obtained with a yield of more than 62.7% under the optimum conditions. The producing process is easy to control with high yield and low cost, and it is suitable for industrial production. The structure of compound 1 was confirmed with1 H NMR, MS, IR,13 C NMR and melting points.

关 键 词：噻萘普汀 中间体 合成 二硫醚 

分 类 号：O649[理学—物理化学]