Molecular Design and Synthesis of Biologically Important Substances

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。利用有机铅试剂和不对称催化反应等有机金属化合物开发新的合成反应。在开发重要生物物质方面，我们成功地合成了异碳环素，这是最有前途的前列环素类似物。6-异ocarbacyclin，预期其拮抗活性，已成为结构-活性关系研究的另一个目标。因此，我们完成了它的外消旋和旋光形式的合成。生物学评价目前正在进行中。有机铅试剂将成为合成有机反应的有用工具。其中一个重要的课题必须是在PG合成中直接引入PG - omega链到-酮酯。在Pinhey的工作基础上，经过多次试验，建立了一种新的合成方法，用于α - (E & Z) -1-烯基酮的一般程序，并结合了有效的脱羧反应。用同样的方法也开发了多用途合成α -炔基酮的方法。开发一种高效、立体选择性、通用性强的糖苷化反应是糖化学研究的重要课题之一。我们现在用糖苷化的新概念挑战一种新的方法。利用Pd （II）催化反应可以有效地将糖转化为合成有用的中间体。

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.