螺异噁唑啉类化合物的合成及生物活性的研究进展

doi:10.6023/cjoc201708013

摘要/Abstract

螺异噁唑啉类化合物具有广泛的生物活性，它们是重要的药物中间体，也是重要的有机合成中间体.综述了四十多年来该类化合物的相关报道，依据反应机理，将螺异噁唑啉类化合物的合成方法归纳为以下五种：氧化法、分子内缩合法、亲核加成法、1，3-偶极环加成法和其他方法.其中，应用最广泛的是1，3-偶极环加成法，该方法操作简单、产率高、立体选择性好，但它的合成子环外双键化合物不易获得，一般要经过多步反应才能制备.另外，还将螺异噁唑啉类化合物的生物活性归纳为以下六类：抑制幼虫生长的活性、延缓动脉硬化的活性、治疗疼痛的活性、降低血糖的活性、抗癌的活性、抗菌的活性.

关键词: 螺异噁唑啉, 合成方法, 生物活性

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

引用此文

李明辉, 松布尔, 穆赫塔尔·伊米尔艾山. 螺异噁唑啉类化合物的合成及生物活性的研究进展[J]. 有机化学, 2018, 38(2): 378-400.

Li Minghui, Song Buer, Imerhasan Mukhtar. Progress in Synthesis and Bioactivity of Spiroisoxazoline Compounds[J]. Chin. J. Org. Chem., 2018, 38(2): 378-400.

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