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Synthetic Studies of Polycyclic Natural Product Stemofoline and Its SAR Study

多环天然产物百叶草碱的合成研究及其比吸收率研究

基本信息

批准号：
23590003
负责人：
SHIMOKAWA Jun
金额：
$ 3.41万
依托单位：
Nagoya University (2012-2013)The University of Tokyo (2011)
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2011
资助国家：
日本
起止时间：
2011 至 2013
项目状态：
已结题

项目摘要

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.

Stemofoline被称为乙酰胆碱酯酶抑制剂，因此它被称为阿尔茨海默病的有效治疗。结构-活性关系研究表明，分子的整体结构对乙酰胆碱酯酶抑制活性很重要。我们开始了对该分子的合成研究，试图合成stemofolines的各种衍生物，这些衍生物不能通过采用天然产物降解物的半合成方法获得。结果，通过分子内1，3-偶极环加成和分子内硅拉-Pummerer反应的结合，以前所未有的环化模式构建了stemofoline的中心多环结构。