2013 Fiscal Year Final Research Report
Synthetic Studies of Polycyclic Natural Product Stemofoline and Its SAR Study
| Project/Area Number |
23590003
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Nagoya University (2012-2013)
The University of Tokyo (2011) |
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Principal Investigator |
SHIMOKAWA Jun 名古屋大学, 創薬科学研究科, 助教 (60431889)
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| Project Period (FY) |
2011 – 2013
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| Keywords | 合成化学 / 天然物全合成 |
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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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