Molecular Design and Synthesis of Biologically Important Substances

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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.