节点文献
茜素S衍生物PGMI-004A的合成
Synthesis of alizarin S derivative PGMI-004A
【摘要】 描述了一种有效合成抗肿瘤活性分子PGMI-004A的新方法。所提出的策略采用亚甲基作为邻苯二酚的保护基团,避免了羟基被氧化的同时解决了中间体的纯化问题。以茜素为原料经过溴代、上保护、磺酰化、偶联、脱保护等5步反应得到目标化合物,总收率达到13.07%。核磁表征结果与文献一致。
【Abstract】 A new method for the efficient synthesis of the antitumor active molecule PGMI-004A was described.The proposed strategy used a methylene group as a protecting group for catechol, which avoid the oxidation of the hydroxyl group and solves the purification problem of the intermediate.The target compound was synthesized from the alizarin by bromination, upper protection, sulfonylation, coupling and deprotection with a total of 13.07%.The nucleomagnetic characterization was consistent with the literature.
【关键词】 合成;
磺酰化;
亚甲基保护基;
PGMI-004A;
【Key words】 synthesis; sulfonylation; methylene protecting group; PGMI-004A;
【Key words】 synthesis; sulfonylation; methylene protecting group; PGMI-004A;
- 【文献出处】 应用化工 ,Applied Chemical Industry , 编辑部邮箱 ,2020年S1期
- 【分类号】TQ460.1
- 【下载频次】1