有机化学 ›› 2008, Vol. 28 ›› Issue (06): 1092-1096. 上一篇    下一篇

研究简报

新型3-萘基-1,3-噻唑烷-4-酮衍生物的微波促进合成及其抗菌活性研究

陈华a,白洁a,赵莲a,苑香果a,李小六*,a,曹克强b   

  1. (<i><sup>a</sup></i>河北大学化学与环境科学学院 保定 071002)<br>(<i><sup>b</sup></i>河北农业大学植物保护学院 保定 071001)
  • 收稿日期:2007-09-26 修回日期:2007-11-07 发布日期:2008-06-26
  • 通讯作者: 李小六

Microwave Assisted Synthesis and Antibacterial Study of 3-Naphthyl-2-[(un)substituted phenyl]-1,3-thiazolidin-4-ones

CHEN Huaa,BAI, Jiea,ZHAO Liana,YUAN Xiang-Guoa,LI Xiao-Liu*a,CAO Ke-Qiangb   

  1. (<i><sup>a</sup> College of Chemistry and Environmental Science</i>, <I>Hebei University</i>, <I>Baoding 071002</i>)<br>(<i><sup>b</sup></i> <I>College of<b> </b>Plant Protection</i>, <I>Hebei<b> </b>Agricultural University</i>, <I>Baoding 071001</i>)<i>
  • Received:2007-09-26 Revised:2007-11-07 Published:2008-06-26
  • Contact: LI Xiao-Liu

利用微波促进的多组分一锅法, 在封管条件下, 以萘胺、芳醛和巯基乙酸为原料, 4-二甲氨基吡啶(DMAP)/<I>N</I>,<I>N</I>’-二环已基碳二亚胺(DCC)为催化剂, 合成了系列新的噻唑烷酮衍生物, 该反应具有时间短、操作简便等优点. 目标化合物通过IR, NMR, MS和元素分析等方法确定结构. 初步测试了化合物对丁香假单胞杆菌黄瓜角斑病菌致病变种、番茄灰霉病菌和黄瓜白粉病菌抑制活性, 结果表明: 部分化合物对黄瓜白粉病菌有显著抑制作用, 但对前两种植物病菌抑制效果不明显.

关键词: 微波促进, 噻唑烷-4-酮, 抗菌活性

A series of 3-naphthyl-2-[(un)substituted phenyl]-1,3-thiazolidin-4-ones were synthesized by the three-component one-pot cyclocondensation of naphthylamine, aromatic aldehyde and 2-mercaptoacetic acid using a microwave-assisted method in the presence of DMAP/DCC. This reaction has such advantages as short reaction time, simple procedure and mild condition. The structures of the synthesized compounds were confirmed by IR, NMR, MS spectra and elemental analysis. Antibacterial (<I>Pseudomonas springae </i>pv. <i>lachrymans</i> (Smith et Bryan) Young, Dye & Wilkie, <I>Botrytis cinerea </i>Pers<i>.</i>, and <I>Sphaerotheca fusca </i>Blum<i>.</i>) activities of the compounds were evaluated, and some of them showed notable inhibition against <I>Sphaerotheca fusca </i>Blum<i>.

Key words: thiazolidin-4-one, antibacterial activity, microwave-assisted