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-phenylsulphonamide)benzoate

作　　者：林润锋[1] 张珩[1] 杨艺虹[1] 张春雷[1] 杨建设[1] 

机构地区：[1]武汉工程大学绿色化工过程省部共建教育部重点实验室,湖北武汉430074

出　　处：《武汉工程大学学报》2009年第12期5-7,共3页Journal of Wuhan Institute of Technology

基　　金：2008年度湖北省教育厅科研项目(B20081504)

摘　　要：以4-氨基甲苯-2-磺酸(Ⅱ)为起始原料,经重氮化—Sandmeyer反应,氧化,酯化,氯磺化,缩合和甲基化六步反应合成4-氯-2-(N-甲基-N-苯基胺磺酰基)苯甲酸甲酯(Ⅰ),总收率高达44.2%.本合成工艺能有效提高反应收率,降低生产成本,适合工业化生产.I的结构经1H-NMRI、R和MS确证.Methyl 4-chloro-2-（N-methyl-N-phenylsulphonamide） benzoate （Ⅰ） was an important intermediate of Tianeptine. Starting with 4-Amino-methylbenzene-2-sulfonic acid （Ⅱ）, the title compound was prepared through diazotization and Sandmeyer reaction, oxidation, esterification, chlorination, condensation and methylation. The total yield was 44.2 %. The improved process was more suitable for industrial production because of higher yield and lower cost. Structure of product was confirmed by IR, MS and ^1H-NMR.

关 键 词：噻萘普汀 Sandmeyer反应 缩合 合成 

分 类 号：O625.523[理学—有机化学]