Synthetic Studies on Biologically Active Substances for Retaining Homeostasis

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A result of our research carried out in 1989-1990 is summarized as follows.1) A new synthetic route to isocarbacyclin which is a potential analogue of prostacyclin discovered in our laboratory was established by employing a C-H insertion reaction of rhodium-carbenoid for the synthesis of a synthetic intermediate and the direct introduction of a omega chain with a 1-alkenyllead reagent for the construction of a secondary synthetic intermediate.2) An improvement of rhodium (II) catalyst for a C-H insertion reaction was studied and a variety of homochiral rhodium carboxylates were prepared for the construction of chiral molecules.3) An efficient and selective synthesis of alpha- (EPSILON and ZETA) -1-alkenyl ketones was established by the combination of a regio- and stereocontrolled introduction of (EPSILON) -1-alkenyl and the corresponding ZETA groups to beta-Keto esters and subsequent reductive removal of ester functionality.4) A higly stereoselective glycosidation by modifying leaving groups involving a phosphorus atom as the best glycosyl donor was extensively studied. The glycosidation method we established was applied to synthesize some anti-tumor agent and further applications are continuously investigated.