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有机化学
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有机化学 ›› 2005, Vol. 25 ›› Issue (08): 954-958. 上一篇    下一篇

研究论文

Aldisin及其衍生物的合成和α-葡萄糖苷酶抑制活性研究

曾向潮*，徐石海，李毅群，王渝芳   

  1. (1 暨南大学化学系 广州 510632)
    (2 中山大学化学与化学工程学院 广州 510275)
  • 收稿日期:2004-07-01 修回日期:2005-03-04 发布日期:2005-07-30
  • 通讯作者: 曾向潮

Syntheses and α-Glucosidase Inhibitions of Aldisin and Its Derivatives

ZENG Xiang-Chao*,XU Shi-Hai,LI Yi-Qun,WANG Yu-Fang   

  1. (1 Department of Chemistry, Jinan University, Guangzhou 510632)
    (2 School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275)
  • Received:2004-07-01 Revised:2005-03-04 Published:2005-07-30
  • Contact: ZENG Xiang-Chao

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以三氯氧磷为环化试剂, 回流状态下, N-(2-吡咯甲酰基)-β-丙氨酸经分子内酰化环化反应, 合成了吡咯[2,3-c]氮杂二酮稠环化合物Aldisin及其衍生物1-Methylaldisin和3-Bromoaldisin, 通过1H NMR, 13C NMR, IR, FABMS和元素分析对其结构进行了表征. 以X射线衍射法研究了3-Methylaldisin的晶体结构. 测定了三个化合物对α-葡萄糖苷酶的抑制作用.

关键词: Aldisin, 1-Methylaldisin, 晶体结构, α-葡萄糖苷酶, 环化反应

Aldisin (6,7-dihydropyrrolo[2,3-c]azepine-4,8(1H,5H)-dione) and its derivatives, 1-methy-
laldisin and 3-bromoaldisin, were synthesized by cyclization of 3-[(pyrrole-2-carbonyl)amino] propionic acids in phosphorus oxychloride under reflux. Their structures were characterized by 1H NMR, 13C NMR, FABMS, IR spectra and elemental analy-sis. The crystal structure of 1-methylaldisin was determined by single-crystal X-ray diffraction. And the α-glucosidase inhibitions of these compounds have also been studied.

Key words: aldisin, cyclization, α-glucosidase, crystal structure, 1-methylaldisin