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Life Function and the Most Advanced Organic Chemistry

生命功能与最先进的有机化学

基本信息

批准号：
61303017
负责人：
OHNO Masaji
金额：
$ 8.32万
依托单位：
University of Tokyo
依托单位国家：
日本
项目类别：
Grant-in-Aid for Co-operative Research (A)
财政年份：
1986
资助国家：
日本
起止时间：
1986 至 1987
项目状态：
已结题

项目摘要

(1) Bioactive compounds with novel structures- Several bioactive natural products have been isolated from marine sponges and octocoral. Cyclonucleosides, (-)-bulgecinine, fumitremergin B, isocarbacyclin and their analogues have synthesized, aiming at new substances with improved bioactivities. A fluoro derivatives of arachidonic acid have been synthesized and its biotransformation was studied. Syntheses of useful ligands for photoaffinity laveling and affinity chromatography of receptors have been examined. Also studied was the chemical modification of DNA which causes mutation.(2) Development of new synthetic methodologies for bioactive molecules - New methods for the deprotection for peptide synthesis and macrolide synthesis have been developed. A new dienophil was invented for C-nucleoside synthesis. Synthesis of vitamine D and related compounds have been studied. Chiral bases, metal complex catalysts, useful methods for asymmetric deprotonation and asymmetric aldol reaction have been applied for natural product synthesis. Polycyclic aromatic compounds and crowned p-benzoquinones have been synthesized and their functions have been investigated. Chiral synthons have been created by enzymatic hydrolysis of symmetric diesters based on the symmetrization-asymmetrization concept.

(1)具有新结构的生物活性化合物-从海绵和珊瑚中分离出几种具有生物活性的天然产物。环己内酯、（-）-bulgecinine、fumitremergin B、isocarbacyclin及其类似物的合成，旨在寻找具有更高生物活性的新化合物。合成了一种含氟的花生四烯酸衍生物，并对其生物转化进行了研究。本文研究了用于光亲和层析和受体亲和层析的配体的合成。还研究了导致突变的DNA化学修饰。(2)生物活性分子合成新方法的发展-发明了一种新的用于C-核苷合成的亲二烯体。研究了维生素D及其相关化合物的合成。手性碱、金属配合物催化剂、不对称去质子化方法和不对称羟醛缩合反应在天然产物合成中得到了广泛的应用。合成了多环芳香族化合物和冠醚对苯醌，并对其功能进行了研究。基于对称化-不对称化的概念，通过酶促水解对称二酯已经产生了手性配体。