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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (9): 1275-1278. 上一篇    下一篇

研究简报

6-氟-4-(N-芳基)胺基喹唑啉类化合物的微波合成及生物活性研究

张培权，宋宝安*，杨松，金林红
胡德禹，刘刚，薛伟   

  1. (a贵州大学精细化工研究开发中心 教育部绿色农药和农业生物工程重点实验室 贵阳 550025)
  • 收稿日期:2005-09-13 修回日期:2006-01-15 发布日期:2006-09-11
  • 通讯作者: 宋宝安

Synthesis and Bioactivity of 6-Fluoro-4-(N-aryl)aminoquinazoline Compounds under Microwave Irradiation

ZHANG Pei-Quan,SONG Bao-An*,YANG Song,JIN Lin-Hong
HU De-Yu,LIU Gang,XUE Wei   

  1. (a Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Research and Development Centre for Fine Chemicals, Guizhou University, Guiyang 550025)
  • Received:2005-09-13 Revised:2006-01-15 Published:2006-09-11
  • Contact: SONG Bao-An

PDF

1327

被引次数

3

经2-氨基-5-氟苯甲酸与甲酰胺闭环、氯化反应, 合成了6-氟-4-氯喹唑啉, 然后在微波辐射下与芳香胺反应, 合成了6个新的6-氟-4-(N-芳基)胺基喹唑啉类化合物. 新化合物经1H NMR, IR及元素分析证明其结构. 体外抑瘤试验证明化合物对前列腺癌细胞(PC3)、人胃癌细胞(BGC823)、人乳腺癌细胞(BCap-37)均无抑制活性. 经ERK的抗磷酸化活性免疫印迹试验证明化合物对小鼠成纤维细胞(NIH3T3)无抑制活性.

关键词: 合成, 微波辐射, 生物活性, 喹唑啉, 氟

Six new 6-fluoro-4-(N-aryl)aminoquinazoline compounds were synthesized, firstly by the cycli-zation reaction of 2-amino-5-fluorobenzoic acid with formamide and then chlorination to attain 4-chloro-6-fluoroquinazoline, finally the amination with arylamines under microwave irradiation. The structures of the six new compounds were characterized by elemental analyses, IR and 1H NMR spectra. Bioactivity of the new compounds was tested. The results showed that the six new compounds had weak anticancer activity to PC3, BGC823, BCap-37 and ERK phosphorylation in NIH3T3 cell induced by PDGF.

Key words: synthesis, microwave irradiation, fluorine, bioactivity, qunazoline