1-(2,4-二氯苯基)-4-甲基-5-(4-氯苯基)吡唑-3-羧酸的新合成方法  

A Novel Synthetic Method for 1-(2,4-Dichlorophenyl)-4-methyl-5-(4-chlorophenyl)-1H-pyrazole-3-carboxylic Acid

作　　者：杨照[1] 王志祥[1] 方正[2] 郭凯[2] 

机构地区：[1]中国药科大学药学院,南京210009 [2]南京工业大学药学院,南京210009

出　　处：《有机化学》2013年第3期607-610,共4页Chinese Journal of Organic Chemistry

基　　金：国家重点基础研究发展计划(973计划;Nos.2012CB725204;2012CB721104)资助项目~~

摘　　要：研究了合成1-(2,4-二氯苯基)-4-甲基-5-(4-氯苯基)吡唑-3-羧酸的新方法.以价廉、易得的对氯苯甲醛为原料,经羟醛缩合、环合及氧化得目标化合物,合成总收率为50.6%.中间体及最终产物结构由1H NMR,MS确证.该方法步骤较少、操作简便、收率良好,是一条适合中试放大的新合成工艺路线.A novel method for the synthesis of 1-（2,4-dichlorophenyl）-4-methyl-5-（4-chlorophenyl）-lH-pyrazole-3-carbox- ylic acid was reported. The target compound was prepared starting from 4-chlorobenzaldehyde, which is inexpensive and eas- ily available starting material, via adol condensation, cyclization and oxidation with the total yield of 50.6%. The structures of intermediates and final product were determined by 1H NMR and MS. The novel method with the advantages of shorten proc- ess, easily conducted procedure and relatively high yield is suitable for scale-up production.

关 键 词：1 5-二芳基吡唑 苯腙 环合 氧化 合成 

分 类 号：TQ463[化学工程—制药化工]