TEMPLATE DIRECTED COMBINATORIAL SYNTHESIS

这个项目的目标是设计和发现新的 用于对映选择性有机合成的催化剂体系 Diels-Alder反应的外选择性催化剂。一个平行的 目标是创建一种新的方法来生成 催化剂等组合化学的靶标。基于 有机分子的分子识别研究 抗体催化的进展，分子库将是 它们是为催化活性而预先组织的。这个 库将通过添加不同的池来合成 添加到受支持化合物中的构建块将是 模板化通过与模拟过渡态的化合物的结合 感兴趣的人。通过这种方式，最有效的积木 绑定反应过渡态-模拟将在 花费那些效率最低的人。铀的选择性浓缩 潜在的催化剂将允许大量潜在的催化多样性 要抽样的成分，并将添加一定程度的选择和 对合成组合文库的扩增。这些化合物 将对所获得的结合和催化活性进行筛选， 鉴定，并独立合成和表征。基于 已发现的铅结构及其动力学、化学和结构 对催化剂及其底物进行分析，优化后的催化剂 综合了所获得的机械学知识。

The objective of this project is the design and discovery of new catalyst systems for enantioselective organic synthesis, directed toward an exo-selective catalyst of the Diels-Alder reaction. A parallel objective is the creation of a new methodology for the generation of catalysts and other targets of combinatorial chemistry. Based on the molecular recognition studies on organic molecules as well as the advances in antibody catalysis, libraries of molecules will be synthesized which are pre-organized for catalytic activity. The libraries will be synthesized by the addition of diverse pools of building blocks whose addition to the supported compound will be templated via binding to a compound which models the transition state of interest. In this way, the building blocks which most effectively bind the reaction transition state-mimic will be incorporated at the expense of those least effective. The selective enrichment of the potential catalysts will allow a large potential diversity of catalytic compositions to be sampled, and will add a degree of selection and amplification to the synthetic combinatorial library. The compounds obtained will be screened for binding and catalytic activity, identified, and independently synthesized and characterized. Based on the lead structures discovered and the kinetic, chemical and structural analysis of the catalyst and its substrates, optimized catalysts will be synthesized which incorporate the mechanistic knowledge obtained.