3-芳硫基-4-羟基香豆素及其类似物的制备

4-羟基香豆素类化合物与4-羟基喹啉酮类化合物是一类重要的有机杂环化合物,因为其良好的生理活性,被广泛应用于抗菌、抗炎、抗HIV、抗肿瘤等药物结构中。 本文用4-羟基香豆素类化合物或4-羟基喹啉酮类化合物作为底物、以硫磺粉(S)为硫源、以碘苯类衍生物作为芳基源,在氯化铜催化作用下合成了3-芳硫基-4-羟基香豆素类化合物和3-芳硫基-4-羟基喹啉酮类化合物。 该方法使用环境友好的硫磺粉为硫源替代有机硫,操作简单、无污染、成本低廉,为该类化合物的绿色合成提供了新的方案。

Preparation of 3-Arylthio-4-hydroxycoumarin and Its Analogs

4-Hydroxylcoumarin and its analogs are one of the most active classes of heterocyclic compounds. Many of these compounds have been proved to have a wide range of biological and pharmacological activities, such as antibacterial, anti-tumor, anti-HIV. Herein, 3-arylthio-4-hydroxycoumarin and its analogs were synthesized from stable non-toxic 4-hydroxycoumarins, iodobenzenes and sulfur in a cheap and environmentally friendly fashion.