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Abstract <p>5-Methyl-1<i>H</i>-1,2,3-triazole-4-carboxylic acid is of interest as a starting material in the synthesis of biologically active compounds. However, the known methods for its preparation provide low yields and utilize difficult-to-obtain reagents. Herein, we describe a simple method for the synthesis of 5-methyl-1<i>H</i>-1,2,3-triazole-4-carboxylic acid by hydrogenative debenzylation of 1-benzyl-5-methyl-1<i>H</i>-1,2,3-triazole-4-carboxylic acid or debenzylation of ethyl 1-benzyl-5-methyl-1<i>H</i>-1,2,3-triazole-4-carboxylate and subsequent hydrolysis of the resulting NH-triazole. The proposed method affords NH-triazoles in quantitative yield. The structure of the synthesized compounds was confirmed by IR and NMR spectra.</p>

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Efficient Synthesis of 5-Methyl-1H-1,2,3-triazole-4-carboxylic Acid

  • 期刊论文

  • 发表日期：

    2026年3月1日

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  • S. V. Strokova,
  • N. A. Alekseeva,
  • M. A. Lenskii,
  • S. V. Sysolyatin,
  • D. I. Koleno,
  • E. Yu. Shumilova,
  • V. G. Uskov,
  • A. V. Ozhogin,
  • D. V. Korabel’nikov

摘要

Abstract

5-Methyl-1H-1,2,3-triazole-4-carboxylic acid is of interest as a starting material in the synthesis of biologically active compounds. However, the known methods for its preparation provide low yields and utilize difficult-to-obtain reagents. Herein, we describe a simple method for the synthesis of 5-methyl-1H-1,2,3-triazole-4-carboxylic acid by hydrogenative debenzylation of 1-benzyl-5-methyl-1H-1,2,3-triazole-4-carboxylic acid or debenzylation of ethyl 1-benzyl-5-methyl-1H-1,2,3-triazole-4-carboxylate and subsequent hydrolysis of the resulting NH-triazole. The proposed method affords NH-triazoles in quantitative yield. The structure of the synthesized compounds was confirmed by IR and NMR spectra.