Synthetic Studies on Optically Active Substances with Remarkable Bioactivities to Analyze Their Biological Functions

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1. Synthesis of radicicol, acetophthalidin and preussin, which show potent inhibition activities against cell-progression was studied. We could finish the synthesis not only of natural products but also related analogs including biotinylated derivatives. As a result, we found that some analogs of acetophthalidin have the similar activities and also all the possible 8 stereoisomers of preussin have the same activity at the similar level.2. Synthesis of plant-growth regulators, such as jasmonoids, pironetin, specifernin, sorokinianin and so on was also accomplished and SAR studies were performed. In the case of pironetin, one of biotinylated analogs bound selectively with micro tubule and now the study on the analysis of function is underway.3. Synthesis of natural products and analogs related to plant protection and plant nutrition. For example, insect antifeedant is a promising pesticide tolerant to eco-system. We succeeded in the synthesis of azadirachtin B-ring skeleton and also another antifeedant, tanabalin via very efficient scheme. These methodologies would be applied to synthesize related molecules to study their biological activities. Expeditious synthesis of phytosiderophores was developed and the synthesis of analogs was executed to create simpler but better derivatives.4. Synthesis of pyrrolidine and piperidine analogs, such as nectrisine, DAB-1, LAB-1, nojirimycin and their analogs with potent glucosidase inhibitors was achieved.