Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (2): 378-400.DOI: 10.6023/cjoc201708013 Previous Articles     Next Articles



李明辉, 松布尔, 穆赫塔尔·伊米尔艾山   

  1. 新疆大学化学与化工学院 乌鲁木齐 830046
  • 收稿日期:2017-08-08 修回日期:2017-09-12 发布日期:2017-09-19
  • 通讯作者: 穆赫塔尔·伊米尔艾山
  • 基金资助:


Progress in Synthesis and Bioactivity of Spiroisoxazoline Compounds

Li Minghui, Song Buer, Imerhasan Mukhtar   

  1. College of Chemistry and Chemical Engineering, Xinjiang University, Urumqi 830046
  • Received:2017-08-08 Revised:2017-09-12 Published:2017-09-19
  • Contact: 10.6023/cjoc201708013
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21462043, 21062019).

Spiroisoxazoline compounds have so extensive biological activity that they are important drug intermediates, and they are also important organic synthetic intermediates. The relevant reports for forty years are reviewed in this paper. On the basis of reaction mechanisms, the synthetic methods of spiroisoxazoline compounds are classified into the following five types:oxidation, intramolecular condensation, nucleophilic addition, 1, 3-dipolar cycloaddition, and other methods. Among them, the most widely used method is 1, 3-dipolar cycloadditio. This method is of simple operation, high yield and good stereoselectivity, but one of its synthons-carbon dipolarophiles is not easy to get, and generally goes through many steps of reaction to prepare. In addition, their biological activities are summarized as six categories:the activity of inhibiting the growth of the larvae, the activity of slowing hardening of the arteries, the activity for the treatment of pain, the activity of lowering blood sugar, the anticancer activity and the antibacterial activity.

Key words: spiroisoxazoline, synthetic method, biological activity