Department of Chemistry, Tamkang University, Tamsui Dist., 25137 New Taipei City, Taiwan.
Molecules. 2012 Jul 9;17(7):8206-16. doi: 10.3390/molecules17078206.
We described herein a concise synthesis of 3',4'-diaminoflavone 10. This new, three-step synthetic approach is more efficient than the conventional seven-step synthetic method. The route is shortened significantly by introducing the amino moieties early and eliminating the need for nitro group reduction. The other two analogues, 5,7-dihydroxy-3',4'-diaminoflavone 11 and 5,7-dimethoxy-3',4'-diaminoflavone 12, were also synthesized similarly. The above three compounds, along with flavone, were evaluated for their antioxidant and UVB-protection abilities on zebrafish larvae. The data showed that compound 10 exhibited the best result, with -102.3% of ROS-scavenging rate.
我们在此描述了 3',4'-二氨基黄酮 10 的简洁合成方法。这种新的三步合成方法比传统的七步合成方法更有效。通过尽早引入氨基部分并消除对硝基还原的需求,路线大大缩短。另外两个类似物,5,7-二羟基-3',4'-二氨基黄酮 11 和 5,7-二甲氧基-3',4'-二氨基黄酮 12,也以类似的方式合成。上述三种化合物与黄酮一起,在斑马鱼幼虫上评估了它们的抗氧化和 UVB 保护能力。数据表明,化合物 10 表现出最好的结果,具有 -102.3%的 ROS 清除率。