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发明授权
CN106496153B 一种1，3-恶唑-2-硫酮类神经氨酸酶抑制剂及其制备方法 有权 转让

一种1，3-恶唑-2-硫酮类神经氨酸酶抑制剂及其制备方法
摘要：
本发明公开了一种1，3‑恶唑‑2‑硫酮类神经氨酸酶抑制剂及其制备方法。本发明的方法具体如下：（1）将芳香醛ArCHO和高氯酸锂LiClO4·3H2O、三甲基氰硅烷TMSCN反应得到氰基类似物；（2）将氰基类似物还原得到2‑羟基胺类化合物；（3）2‑羟基胺类化合物、二硫化碳和硝酸铅反应得到1，3‑恶唑‑2‑硫酮中间体；（4）碱性条件下，1，3‑恶唑‑2‑硫酮中间体与亲核试剂反应得N‑取代的1，3‑恶唑‑2‑硫酮类神经氨酸酶抑制剂。本发明得到的抑制剂展现出了较好的神经氨酸酶抑制活性，IC50值可达到16μM。同时，本发明合成方法简单，所用原料廉价易得。
摘要（英）：

The invention discloses a 1,3-oxazole-2-thioketone neuraminidase inhibitor and a preparation method thereof. The method comprises the following concrete steps: (1) reacting aromatic aldehyde ArCHO with lithium perchlorate LiClO4.3H2O and trimethylsilyl cyanide TMSC so as to obtain a cyan analog; (2) reducing the cyan analog so as to obtain a 2-hydramine compound; (3) reacting the 2-hydramine compound with carbon disulfide and lead nitrate so as to obtain a 1,3-oxazole-2-thioketone intermediate; and (4) subjecting the 1,3-oxazole-2-thioketone intermediate and a nucleophilic reagent to a reaction under an alkaline condition so as to obtain the N-substituted 1,3-oxazole-2-thioketone neuraminidase inhibitor. The inhibitor prepared in the invention presents good neuraminidase inhibition activity and has an IC50 value of 16 [mu]M. Meanwhile, the preparation method is simple and uses cheap and easily available raw materials.

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