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有机化学
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有机化学 ›› 2014, Vol. 34 ›› Issue (10): 2146-2151.DOI: 10.6023/cjoc201404049 上一篇    下一篇

研究简报

2,6,6-三甲基-双环[3,1,1]庚基-3-(4-芳基-2-噻唑)腙类化合物的合成及其抑菌和抗肿瘤活性研究

鲍名凯a, 杨益琴b, 谷文a, 徐徐a, 曹明珍a, 王石发a,c   

  1. a. 南京林业大学化学工程学院 南京 210037;
    b. 南京林业大学轻工科学与工程学院 南京 210037;
    c. 江苏省生物质绿色燃料与化学品重点实验室 南京 210037
  • 收稿日期:2014-04-26 修回日期:2014-05-22 发布日期:2014-06-11
  • 通讯作者: 王石发 E-mail:wsfyyq@njfu.com.cn
  • 基金资助:

    国家自然科学基金（No. 31170538）、江苏省教育厅优势学科经费（No. 201104015）资助项目.

Synthesis and Antibacterial, Antitumor Activity of 2,6,6-Thrimethyl- bicyclo[3,1,1]heptan-3-(4-aryl-2-thiazoyl)hydrazones

Bao Mingkaia, Yang Yiqingb, Gu Wena, Xu Xua, Cao Mingzhena, Wang Shifaa,c   

  1. a. College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037;
    b. College of Light Industry and Engineering, Nanjing Forestry University, Nanjing 210037;
    c. Jiangsu Key Laboratory of Biomass-based Green Fuels and Chemicals, Nanjing 210037
  • Received:2014-04-26 Revised:2014-05-22 Published:2014-06-11
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 31170538) and the Forestry Public Sector Research Found of State Forestry Administration of China (No. 201104015)

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被引次数

2

以α-蒎烯为起始原料，经加成、氧化、缩合制得中间体，继而与α-溴代芳基乙酮在常温下反应合成12个新型2，6，6-三甲基-双环[3，1，1]庚基-3-（4-芳基-2-噻唑）腙类化合物，产率达52.4%～88.9%. 其结构经1H NMR，13C NMR，IR，LC/MS和元素分析进行了确证. 初步生物活性测试结果表明：部分目标化合物具有较好的抑菌活性和一定的抗肿瘤活性.

关键词: 庚基-3-(4-芳基-2-噻唑)腙, 合成, 抑菌活性, 抗肿瘤活性

Twelve new 2,6,6-thrimethyl-bicyclo[3,1,1]heptan-3-(4-aryl-2-thiazoyl)hydrazones were synthesized by using α-pinene as starting material in four steps reaction including addition, oxidation, condensation, and reaction with α-bromo- acetophenone under room temperature. The yields of products were in the range from 52.4% to 88.9%. All synthesized new compounds were confirmed by 1H NMR, 13C NMR, IR, LC/MS spectra and elemental analysis. The preliminary bioassay showed that some of the target compounds exhibited significant antibacterial activity and certain antitumor activity.

Key words: heptan-3-(4-aryl-2-thiazoyl)hydrazone, synthesis, antibacterial activity, antitumor activity