Development of new Synthons, Catalysts and Applications in Organic Synthesis

这一研究项目关注的是利用相对便宜的、可用的烯烃和烯烃衍生物等基本化学物质，利用过渡金属催化和有机催化等催化技术，利用不对称环加成反应将这些基本化学物质转化为高价值的手性中间体的方法的发展。这些反应的产物可直接用作或可方便地转化为具有生物活性的天然产物和/或其衍生物。***包括但不限于抗癌剂、抗病毒剂、抗寄生虫剂。除了这些应用方面之外，环丁烷、环戊烷和环己烷的一般合成也具有普遍重要性，因为这些核心特征在天然和非天然有机化合物的光谱中以及在材料中都存在。将详细研究获取核心分子手性功能化版本的方法。这里开发的方法允许以不对称的方式访问每个核心的高度功能化变化，因此这项工作对于推进适用于许多领域的合成方法具有普遍重要性。该方法的应用包括为加拿大工业生产的基本化学品开辟途径，并将该方法应用于超出赠款范围的各种领域的高价值药品。这一领域的工作可以培训高素质的研究人员，以获得技能和经验，并将这些技能转化为对他们有很高需求的工业、学术和机构。

This program of research concerns the development of methods that utilize relatively inexpensive, available building block chemicals known as olefins and olefin derivatives, using catalytic techniques, such as transition metal catalysis and organocatalysis, and to convert these building blocks to high value chiral intermediates using asymmetric cycloaddition reactions. The products of these reactions are either directly useful as, or may be conveniently converted to, biologically active natural products and/or derivatives thereof.***These include, but are not limited to, anticancer agents, antiviral agents, anti-parasitic agents. In addition to these applied aspects, the general synthesis of cyclobutanes, cyclpentanes and cyclohexanes is of general importance in view of the occurrence of these core features across the spectrum of natural and non-natural organic compounds and in materials. The methods to access chiral functionalized versions of the core molecules will be researched in detail. The methods developed here allow access to highly functionalized variations of each core in and asymmetric fashion and hence the work is of general importance in advancing synthetic methodology applicable to many fields. Applications of the methodology include opening routes to building block chemicals produced by Canadian industry and applications of the methods apply to high-value pharmaceuticals of use in a variety of areas extending beyond the scope of the grant. Work in this area allows for the training of highly qualified researchers to gain skills and experience and to translate those skills to industrial, academic and institutions where they are in very high demand.