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有机化学
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有机化学 ›› 2013, Vol. 33 ›› Issue (03): 607-610.DOI: 10.6023/cjoc201210032 上一篇    下一篇

研究论文

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

杨照a, 王志祥a, 方正b, 郭凯b   

  1. a 中国药科大学药学院 南京 210009;
    b 南京工业大学药学院 南京 210009
  • 收稿日期:2012-10-17 修回日期:2012-11-23 发布日期:2012-11-26
  • 通讯作者: 王志祥 E-mail:zhixwang@163.com
  • 基金资助:

    国家重点基础研究发展计划(973计划, Nos. 2012CB725204, 2012CB721104)资助项目.

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

Yang Zhaoa, Wang Zhixianga, Fang Zhengb, Guo Kaib   

  1. a College of Pharmacy, China Pharmaceutical of University, Nanjing 210009;
    b School of Pharmaceutical Science, Nanjing University of Technology, Nanjing 210009
  • Received:2012-10-17 Revised:2012-11-23 Published:2012-11-26
  • Supported by:

    Project supported by the National Key Basic Research Program of China (973 Program) (Nos. 2012CB725204, 2012CB721104).

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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)-1H-pyrazole-3-carbox- ylic acid was reported. The target compound was prepared starting from 4-chlorobenzaldehyde, which is inexpensive and easily 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 process, easily conducted procedure and relatively high yield is suitable for scale-up production.

Key words: 1,5-diarylpyrazole, phenyl hydrazone, cyclization, oxidation, synthesis