高等学校化学学报

高等学校化学学报 ›› 2000, Vol. 21 ›› Issue (S1): 452.

• Synthetic Sciences • 上一篇    下一篇

Synthesis of 1-aryl-5-methyl-4-substituted-l,2,3-triazoles

ZHANG Yan, CHU Chang-Hu, QIAO Ren-Zhong, XU Peng-Fei, ZHANG Zi-Yi   

  1. Dept. of Chemistry, National Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou
  • 出版日期:2000-12-31 发布日期:2000-12-31
  • 基金资助:

    This project is supported by NNSF of P. R. China.

Synthesis of 1-aryl-5-methyl-4-substituted-l,2,3-triazoles

ZHANG Yan, CHU Chang-Hu, QIAO Ren-Zhong, XU Peng-Fei, ZHANG Zi-Yi   

  1. Dept. of Chemistry, National Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou
  • Online:2000-12-31 Published:2000-12-31
  • Supported by:

    This project is supported by NNSF of P. R. China.

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摘要：

As 1-aryl-5-methyl-4-substituted-1,2,3-triazoles often exhibit broad spectrum biological actions, we have synthesized many heterocyclic and condensed heterocyclic compounds which contained 1-aryl-5-methyl-1,2,3-triazol-4-yl functional groups and screened their antibacterical activities[1,2]. Our further work testified that it was necessary to go on studying such kind of compounds. In order to improve the soluble of these compounds, we chose aniline and p-toluidime as starting materials to synthesize 1-aryl-5-methyl-4-substituted-1,2,3-triazoles 1a-b, 2a-b, 3a-b, 4a-b, 5a, These new compounds all have active reaction groups such as SH, NH2 as well as OH. So they might react with ω-substituted-ω-bromo-acetophenone and 6a-b, 7a-b, 8a-b, 9a were obtained. They are all soluble in hot alcohol. Under similar conditions it is difficult to let 4a-b react completely with ω-substituted-ω-bromo-acetophenone. We only observed a little new compounds by TLC. By Mannich reaction, 1a-b also could react with formaldelyde and p-toluidime and l0a-b were isolated. The evaluation of the biological activity is in progress.

Abstract:

As 1-aryl-5-methyl-4-substituted-1,2,3-triazoles often exhibit broad spectrum biological actions, we have synthesized many heterocyclic and condensed heterocyclic compounds which contained 1-aryl-5-methyl-1,2,3-triazol-4-yl functional groups and screened their antibacterical activities[1,2]. Our further work testified that it was necessary to go on studying such kind of compounds. In order to improve the soluble of these compounds, we chose aniline and p-toluidime as starting materials to synthesize 1-aryl-5-methyl-4-substituted-1,2,3-triazoles 1a-b, 2a-b, 3a-b, 4a-b, 5a, These new compounds all have active reaction groups such as SH, NH2 as well as OH. So they might react with ω-substituted-ω-bromo-acetophenone and 6a-b, 7a-b, 8a-b, 9a were obtained. They are all soluble in hot alcohol. Under similar conditions it is difficult to let 4a-b react completely with ω-substituted-ω-bromo-acetophenone. We only observed a little new compounds by TLC. By Mannich reaction, 1a-b also could react with formaldelyde and p-toluidime and l0a-b were isolated. The evaluation of the biological activity is in progress.

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