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发明授权
CN106632285B 一种齐多夫定-1,2,3-三氮唑类化合物的合成方法 有权

一种齐多夫定-1,2,3-三氮唑类化合物的合成方法
摘要：
本发明公开了一种齐多夫定‑1,2,3‑三氮唑类化合物的合成方法，属于具有抗菌活性药物的合成技术领域。本发明的技术方案要点为：一种齐多夫定‑1,2,3‑三氮唑类化合物的合成方法，具体合成路线为：。本发明根据齐多夫定分子中含有叠氮基团，通过click反应使其与带有不同取代基的苯胺基丙炔类化合物反应得到齐多夫定‑1,2,3‑三氮唑类化合物，并且选择革兰氏阳性菌‑金黄葡萄球菌、革兰氏阴性菌‑大肠杆菌和真菌‑白色念珠球菌对所合成的齐多夫定‑1,2,3‑三氮唑类化合物进行了体外抗菌活性测定，结果表明该类化合物均具有较好的抗菌活性。
摘要（英）：

The invention discloses a method for synthesizing a zidovudine-1,2,3-triazole compound, belonging to the technical field of antibacterial active medicines. According to the technical scheme of the invention, the specific route of the method for synthesizing the zidovudine-1,2,3-triazole compound is as shown in the specification. According to the method, on the basis that zidovudine molecules comprise azide groups, click reaction can be performed to enable zidovudine to react with aniline allylene compounds with different substituent groups so as to obtain the zidovudine-1,2,3-triazole compound, moreover gram-positive bacterium-staphylococcus aureus, gram-negative bacterium-escherichia coli and fungus-candida albicans are selected to perform in-vitro antibacterial activity testing on the zidovudine-1,2,3-triazole compound, and the results show that the compound has relatively good antibacterial activity.

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