Molecular Design and Synthesis of Biologically Important Substances

重要生物学物质的分子设计与合成

基本信息

批准号：
05453184
负责人：
IKEGAMI Shiro
金额：
$ 4.61万
依托单位：
Teikyo University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1993
资助国家：
日本
起止时间：
1993 至 1994
项目状态：
已结题

项目摘要

Our major research projects concerm the molecular design of biologically useful and important substances related to the endogenous substances and their synthesis and biological evaluations. Development of new synthetic reactions using oarganometallics such as organolead reagents and asymmetric catalytic reactions is also involved.1. In connection of exploiting biologically important substances, we succeeded in the synthesis of Isocarbacyclin which is most promising prostacyclin analogue as new drug. 6-Isocarbacyclin, which will be expected as its antagonistic activity, has been another target for examination of the styuctureactivity relationship. Thus, we accomplished the synthesis of it as racemic and optically active forms. Biological evaluation is currently under a way.2. Organolead reagents will be useful tools for synthetic organic reactions. One of the inportant subject must be the direct introduction of PG omega-chain to beta-keto esters in PG synthesis. After many trials of the reactions based on Pinhey's work, new synthetic methodology for the general procedure of alpha- (E & Z) -1-alkenyl ketons has been established with the combined operation of an efficient decarboxylation reaction. The versatile synthetic method of alpha-alkynyl ketones has also been developed with the similar manner.3. One of key subjects in sugar chemistry must be the development of an efficient and stereoselective glycosidation which is high versatility with a wide range of applicability. We are challenging now a new methodology with new concepts of glycosidation. An efficient transformation of sugars into synthetically useful intermediates could be developed by employing Pd (II) catalyzed reaction.

我们的主要研究项目让您的生物学上有用和重要物质的分子设计与内源性物质及其合成和生物学评估有关。还涉及使用橡子仪的新合成反应开发新的合成反应，例如有机脂肪试剂和不对称的催化反应。1。在利用生物学上重要的物质方面，我们成功地合成了异含素蛋白，这是最有希望的前列环素类似物作为新药。 6-异育糖环蛋白将被认为是其拮抗活性，它是检查造型性关系关系的另一个目标。因此，我们将其合成为外消旋和光学活性形式。生物学评估目前处于某种方式下。2。 Organolead试剂将是合成有机反应的有用工具。不重要的主题之一必须是将PG欧米茄链直接引入PG合成中的β-酮酯。经过基于Pinhey的工作的反应进行了多次试验，已建立了用于α-（E＆Z）-1-烷基酮的一般程序的新合成方法，并通过有效的脱羧反应的合并操作建立了。 α-碱基酮的多功能合成方法也以类似的方式开发了3。糖化学的关键主题之一必须是开发有效和立体选择性的糖苷，该糖苷具有很高的多功能性，具有广泛的适用性。现在，我们正在挑战一种新方法，并具有新的糖化概念。可以通过采用PD（II）催化反应来开发糖向合成有用的中间体的有效转化。