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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (07): 870-873. 上一篇    下一篇

研究简报

(S)-萘普生-1,4-二氢吡啶类化合物的合成与生物活性

胡艾希*，谢艳丽，伍小云，叶姣   

  1. (a湖南大学化学化工学院 长沙 410082)
    (b南方医科大学药学院 广州 510515)
  • 收稿日期:2006-03-27 修回日期:1900-01-01 发布日期:2007-06-30
  • 通讯作者: 胡艾希*

Synthesis and Bioactivity of 1,4-Dihydropyridine Moiety Substituted (S)-Naproxen

HU Ai-Xi*,XIE Yan-Li,WU Xiao-Yun,YE Jiao   

  1. (a College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082)
    (b College of Pharmaceutical Sciences, South Medical University, Guang-zhou 510515)
  • Received:2006-03-27 Revised:1900-01-01 Published:2007-06-30
  • Contact: HU Ai-Xi*

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以(S)-萘普生为原料制得的(S)-萘普生氯甲酯与1,4-二氢吡啶-3,5-二羧酸单酯在无水K2CO3存在下于DMF中反应得到的粗产品经梯度结晶或柱层析纯化得标题化合物. 合成的7种目标化合物收率21%～73%, 经1H NMR, IR, MS确证了结构. 家兔离体血管平滑肌收缩试验研究表明, 大部分目标化合物对苯肾上腺素诱导的血管收缩有松弛作用.

关键词: (S)-萘普生-1,4-二氢吡啶类化合物, 合成, 生物活性

The target compounds were synthesized by the reaction chloromethyl ester of (S)-naproxen with 1,4-dihydropyridine-3,5-dicarboxylic monoester in DMF in the presence of K2CO3, and purified by gradient crystallization or column chromatography on silica gel. The yields of seven new compounds were 21%～73%. The structures of the compounds were confirmed by 1H NMR, IR and MS spectra. The effect of such new compounds on the contrac-tion of aorta smooth muscle was observed on the isolated arotic strips of rabbits, and most of them could re-lax constricting strip induced by phenylephrine.

Key words: synthesis, bioactivity, 1,4-dihydropyridine moiety substituted (S)-naproxen