| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2012: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2011: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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| Research Abstract |
Stemofoline is known as a Acetylcholine esterase inhibitor, and thus it is known as the potent cure for Alzheimer disease. Structure-activity relationship study performed thus far indicated that the whole structure of the molecule is important for the Acetylcholine esterase inhibition activity. We started our synthetic study for this molecule in an attempt to synthesize various derivatives of stemofolines that could not be accessed by the semisynthetic approach employing the degradate of the natural product. As a result, construction of the central polycyclic structure of stemofoline was achieved by the combination of the intramolecular 1,3-dipolar cycloaddition and intramolecular sila-Pummerer reaction, with an unprecedented mode of cyclization.
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