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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涉及与内源性物质相关的生物有用和重要物质的分子设计及其合成和生物学评价。还涉及到有机金属化合物的新合成反应如有机铅试剂和不对称催化反应的发展.结合生物活性物质的开发，我们成功地合成了最有前途的前列环素类似物--异碳环素。预期具有拮抗活性的6-异碳环素已成为检查结构反应性关系的另一个目标。因此，我们完成了它的外消旋和光学活性形式的合成。目前正在进行生物学评价。有机铅试剂将成为有机合成反应的有用工具。将PG的ω链直接引入到β-酮酸酯的合成中是今后研究的重要课题之一。在Pinhey工作的基础上，经过多次反应试验，已经建立了α-（E & Z）-1-烯基酮的一般程序的新合成方法，并结合了有效的脱羧反应。α-炔基酮的通用合成方法也以类似的方式发展.糖化学中的关键课题之一必须是开发高效和立体选择性的糖苷化，其具有高度的通用性和广泛的适用性。我们现在正在用糖苷化的新概念挑战新方法。利用Pd（II）催化的反应可以有效地将糖转化为合成有用的中间体。