一种新型的具有潜在抗艾滋病活性药物的合成方法

One synthesis method of a novel potential-active anti-AIDS drug

目的合成一种具有潜在抗艾活性的蛋白酶抑制剂类抗艾滋病药物,并对其可能的合成路线进行相应的讨论。方法以S-(-)-苹果酸为原料,经过缩醛化,亲核取代,还原,氧化,还原胺化,水解等六步反应后,最终得到高ee值的具有潜在抗艾滋病活性的化合物。结果所得产物经1H-NMR检测确定为目标化合物,且纯度大于98%。结论以S-(-)-苹果酸为原料,经过六步反应成功合成了高ee值的目标化合物,经1H-NMR确定结构正确,从而确定了该化合物合成路线的可行性。

Objective To prepare a novel and potential anti - AIDS drug and discuss its possible synthetic route. Methods Using S - （ - ） - malic acid as raw material,the anti - AIDS drug with high ee value was obtained through acetalization,nucle- ophilic substitution, reduction, oxidation, reduction - amination and hydrolysis. Results The product was by l H - NMR, and the compound purity was above 98%. Conclusion The target compound was successfully prepared though 6 steps with its structure conformed by l H - NMR, and the synthetic route was proved reliable.