Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2016: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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Outline of Final Research Achievements |
Ent-kaurenes diterpenoids, isolated from isodon herbs such as Rabdosia japonica, are known to have useful biological activities. In this study, we focus on the total synthesis of ent-kauren-15-ones showing NF-κB inhibitory activity. A tandem cyclization reaction was designed as an efficient method for construction of the kaurene skeleton composed of 6/6/6/5 membered rings including bicyclo [3.2.1] octane. As a result of various synthetic investigations, we have found a method based on an intramolecular tandem radical cyclization reaction using low valence titanium ion.
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