抗骨质疏松药依普黄酮的合成

SYNTHESIS OF IPRIFLAVONE A NEW ANTI-OSTEOPOROSIS IPRIFLAVONE DRUG

目的合成制备新型抗骨质疏松药依普黄酮 ,改进产品及中间体的合成和纯化工艺条件。方法以间苯二酚和苯乙酸为原料 ,经酰化、环合及醚化三步反应进行合成。在酰化反应中 ,探讨了三种原料的摩尔比 ,改进了中间体的分离纯化工艺。在环合反应中 ,选用三氯氧磷和二甲基甲酰胺为环合试剂。结果合成品质量和收率符合文献要求。结论本文报道的合成工艺 ,原料易得、反应条件温和。

ObjectiveTo synthesize Ipriflavone, a ne w anti osteoporosis drug,to improve the condition required for the synthesis and puification of Ipriflavone and intermediates. MethodsThe synthetic route consisted of three steps starting from resorcinol and phenylacetic acid and went through acylation, cyclization, and etherification. Molar ratio of the three raw materials was compared during acylation, and the technique used for the seperation of the intermediates were improved. Phosphorus oxychloride and N,N Dimethylformamide were used as cyclizing agent.ResultsThe quality and yield of Ipriflavone is consist with the data reported in the literature.ConclusionThe raw materials used are commercially available, the reaction conditions are mild, and the process is simple and pratical.