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Investigation of new biologically active compounds containing a dendrimer skeleton

含有树枝状聚合物骨架的新型生物活性化合物的研究

基本信息

批准号：
15550036
负责人：
TSUBOI Sadao
金额：
$ 2.05万
依托单位：
OKAYAMA UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2003
资助国家：
日本
起止时间：
2003 至 2005
项目状态：
已结题

项目摘要

This project consists of investigation of the synthesis of biologically active compounds, which can be utilized for new medicines. These materials have dendrimer skeletone and biologically active components. Research interest of head investigator was the synthesis of biologically active compounds for a long time. Another investigator has developed new chemistry of fullarodendrimers. Head investigator synthesized many oxygen-contaning biologically active compounds such as anticancer and antibiotics by Darzen's condensation (reaction of aldehydes and dichloroacetates in the presence of base) as a key step. In this research, head investigator discovered a new synthetic method of alpha-hydroxy butenolides by the treatment of glycidic esters with MgCl_2, and 3-DPA lactone was prepared. Head investigator found out treatment of alpha-chloroglycidic esters (1) with triphenylphosphine gives 3-chloro-2-ketoesters (2). Furthermore, treatment of 1 with potassium acetate gave 2-acetoxy-3-ketoesters (3) newly. By this new reaction, (-)-verrucosapyrone A (4) was synthesized and the absolute configuration of its one carbon was clarified. The structure of 4 is similar to that of pestalotin, of which has an activity of promotor of plant growth. So, many biological activities would be expected. New pyrone synthesis from acetonide-protected glycidate (1) was also reported.In a future, connection of newly prepared oxygen-containing cyclic compounds with fullarodendrimer will be established, and biological activities of these final products would be investigated.In this project, many new results were obtained and thirteen papers were published in valuable journals.

该项目包括对生物活性化合物的合成进行研究，这些化合物可用于新药。这些材料含有树枝状大分子骨架和生物活性成分。长期以来，首席研究员的研究兴趣主要集中在生物活性化合物的合成上。另一位研究人员开发了富碳树枝状大分子的新化学。首席研究员以达尔岑缩合反应(醛和二氯乙酸酯在碱存在下的反应)为关键步骤合成了许多含氧生物活性化合物，如抗癌和抗生素。本研究发现了用氯化镁处理缩水甘油酸酯合成α-羟基丁烯内酯的新方法，并合成了3-DPA内酯。首席调查员发现，用三苯基膦处理α-氯代缩水甘油酯(1)得到3-氯-2-酮酸酯(2)。此外，1与醋酸钾反应得到了新的2-乙酰氧基-3-酮酯(3)。通过这个新反应，合成了(-)-疣状吡喃酮A(4)，并明确了它的一个碳的绝对构型。4的结构与香豆素相似，具有植物生长促进剂活性。因此，许多生物活动是可以预期的。还报道了丙酮保护的缩水甘油酸酯(1)合成新的吡喃酮。未来将建立新制备的含氧环化合物与富勒树枝状大分子的连接，并对这些最终产物的生物活性进行研究。在本项目中，获得了许多新的结果，并在有价值的期刊上发表了13篇论文。