| Budget Amount *help |
¥16,770,000 (Direct Cost: ¥12,900,000、Indirect Cost: ¥3,870,000)
Fiscal Year 2020: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2019: ¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
Fiscal Year 2018: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Outline of Final Research Achievements |
We have found that novel disaccharide analogues are effective inhibitors of sialidase despite their substrate structure. Conversion to oligosaccharide structure from these analogs is expected to be a more effective inhibitors for sialidases. Therefore, in this study, we worked to establish an efficient synthetic method. Although we could not achieve the site-selective C-H insertion reaction at the C3 position, we succeeded in introducing acetic acid or malonic acid units by oxidative radical coupling, and achieved the modification of C3-position of the sialic acid in only four steps. Furthermore, the results suggest that this route may also improve the efficiency of glycosylation, which was another problem.
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