1.Research About Synthesis And Biological Activity Of Derivatives Of 7-hydroxyl-2-ethyl-4'-methoxyl Isoflavone 2.The Synthetic Technology Improvement Of Diphenylphosphine Oxide

Isoflavone is a group of native compounds which are widely distributed and have various biological activities. It is an effective component of many medicinal plants. Its function in cardiovascular system,endocrine systerm anti -tumor as well as anti-osteoporosis sickness have received extensive recogni -tion. Through Our group's research of its structure decorations, 2-methyl-7-piperidinoethoxyl-4'-hydroxyl isoflavone and 2-ethyl-7-piperidinoethoxyl-4'-hydro xyl isoflavone have been found having an anti-tumor activity.Following the idea of decoration of isoflavone of our research team, two isoflavone compounds with fine biological activity, named 7-hydroxyl isoflavone and 7-hydroxyl-2-ethyl-4'-methoxyl isoflavone were chose to be the parentsubstance in this study. Three base groups-morpholine, piperidine, and adeninewere designed to decrorate the parent substance to be ether in 7 position. Then, the preliminary test of the biological activity of those compounds was carried out.The parent substance was synthesized successfully through the following route. 8 target compounds and their corresponding synthetic routes were designed after review on relevant literatures. The 8 target compounds were synthesized successfully through the routes illustrated in chart 1-2 and chart 1-3. The structure of all obtained compounds was verified by Mp,¹HNMR,¹³CNMR or mass spectrum. In addition, the synthesis of several target compounds (compound 5-8, saw chart 3-2) was improved. And the synthetic technology was simplified, with higher yields.Through the entire process , 18 compounds have been synthesized. Ten of them have never been reported.Moreover, the preliminary test of the biological activity of the 8 target derivatives showed that 7-(2-adenine)ethoxyl-2-ethyl-4'- methoxy isoflavone and 7-(2-hydroxyl-3-piperidino)propoxy-2-ethyl-4'- methoxyl isoflavone have fine biological activities on suppression of the growth of MCF-7 cell in breast cancer and the hela cell in cervical cancer of human being. The diphenylphosphine oxide is an important organic synthesis intermediate. Generally speaking, it usually requests extremely expensive reagents,absolute anhydrous and the non-oxygen condition during the industrial production. These factors make it difficult to carry out its synthesis in large scale.Therefore, to improve the synthesis of diphenylphosphine oxide and develope a simpler and lower cost synthetic route could be practically significant in some way.One-pot method was chose to sythesize diphenylphosphine oxide after review on relevant literature. The specific reaction condition of this method was explored as well. Finally cheaper materials such as PCl₃ benzene and AlCl₃ were used to synthesized this target compound through one-pot method. With this improved method, the synthetic technology was simplified, with a higher yield of 21%. Yet the refining method of target compound requires further study.