| Budget Amount *help |
¥51,870,000 (Direct Cost: ¥39,900,000、Indirect Cost: ¥11,970,000)
Fiscal Year 2015: ¥11,050,000 (Direct Cost: ¥8,500,000、Indirect Cost: ¥2,550,000)
Fiscal Year 2014: ¥11,050,000 (Direct Cost: ¥8,500,000、Indirect Cost: ¥2,550,000)
Fiscal Year 2013: ¥11,700,000 (Direct Cost: ¥9,000,000、Indirect Cost: ¥2,700,000)
Fiscal Year 2012: ¥11,570,000 (Direct Cost: ¥8,900,000、Indirect Cost: ¥2,670,000)
Fiscal Year 2011: ¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
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| Outline of Final Research Achievements |
We have developed organocatalyst bearing guanidine and (thio)urea group, which are linked together through the chiral amino acids linkers. In this research, we have further examined the structure development of the catalysts and have applied the synthesis of natural products and anti-cancer drugs.
First, we have developed asymmetric oxidation of beta-ketoesters bearing tetralone skeleton in the presence of catalyst and CHP. In this reaction, high enantioselectivities were obtained. With the catalysis, daunorubicin and camptothecin were synthesized. This oxidation reaction was then applied to the kinetic resolution version. With the reaction, kinetic resolution took place, and corresponding beta-substituted products were obtained with high selectivity. This reaction was applied to the synthesis of (+)-linoxepin and (+)-rishirilide B. Finally, synthesis of dihydrolycoricidine was achieved based on entropy-dependent Friedel-Crafts reaction in the presence of organocatalyst.
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