有机化学 ›› 2012, Vol. 32 ›› Issue (01): 88-94.DOI: 10.6023/cjoc1107161 上一篇    下一篇

研究论文

新型吡啶-2-酮类衍生物的合成及生物活性

曾永明a, 沈松伟b, 刘方明a,b   

  1. a 新疆大学化学化工学院 乌鲁木齐 830046;
    b 杭州师范大学材料与化学化工学院 杭州 310036
  • 收稿日期:2011-07-16 修回日期:2011-07-30 发布日期:2011-09-27
  • 通讯作者: 曾永明 E-mail:zym903@126.com
  • 基金资助:

    国家自然科学基金(Nos. 29702007, 20162004)资助项目.

Synthesis and Biological Activity of New 5-Heteroaryl-2-pyridone Derivatives

Zeng Yongminga, Shen Songweib, Liu Fangminga,b   

  1. a College of Chemistry and Chemical Engineering, Xinjiang University, Urumqi 830046;
    b College of Materials and Chemical Engineering, Hangzhou Normal University, Hangzhou 310036
  • Received:2011-07-16 Revised:2011-07-30 Published:2011-09-27
  • Contact: Yong-Ming Zeng E-mail:zym903@126.com
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 29702007, 20162004).

以3-氰基-5-乙酰基-6-甲基吡啶-2-酮(1a1b)为原料, 通过多步反应, 合成了18 种未见报道的含有均三唑并[3,4-b][1,3,4]噻二嗪或1,3,4-噁二唑啉的两类新型吡啶酮类化合物4a4h, 7a7j, 其结构经1H NMR, IR 和MS 及元素分析确证. 利用单晶X 射线衍射法测定了化合物4a 的晶体结构. 初步生测表明, 部分化合物表现出不同的抗菌活性.

关键词: 均三唑并[3,4-b][1,3,4]噻二嗪, 1,3,4-噁二唑啉, 晶体结构, 抗菌活性

Eighteen title pyridone compounds containing the 1,3,4-oxadiazoline or 1,3,4-thiadiazine group were synthesized by the multi-step reaction using 5-acetyl-3-cyano-2-methyl-2-pyridone as stating materials. Structures of new compounds were characterized by 1H NMR, IR, MS techniques and elemental analysis. Compound 4a was further studied by single crystal X-ray diffraction analysis. The results of antibacterial activity experiment indicated that all compounds were all resistant to three different bacterias with various degrees.

Key words: 1,3,4-oxadiazoline, s-triazolo[3,4-b][1,3,4]thiadiazine, crystal structure, biological activity