探索羟基在有机小分子催化中的应用

近些年来，尽管有机小分子催化已经得到了迅速的发展，但这一催化领域依然存在着诸多的限制与亟待解决的关键性科学问题：催化活性较低、催化剂用量大以及可调控的发散合成依旧难于实现等。鉴于此，我们以过去的相关研究为基础，设想以羟基为媒介，为解决上述两个核心科学问题提供方案。前期研究发现，在一些有机小分子催化剂和底物中合理的引入羟基，不仅可以大幅提升催化剂和底物的活性，还可以实现可调控的发散合成。因此，拟更加深入系统的探索羟基在有机小分子催化中的应用，本项目将从以下三个方面展开：（1）设计与合成新的含有羟基的双功能催化剂，并探索其应用价值；（2）在吲哚和其它杂环化合物中引入羟基，实现非常规位点的活化和区域选择性发散合成；（3）探索羟基和其它取代基对惰性底物的活化作用。相信这些研究会一定程度上促进有机小分子催化的蓬勃发展与应用。

Despite the rapid development of asymmetric organocatalysis in recent years, there are still some limitations and critical scientific issues to be solved urgently: low catalytic activity, large amount of catalyst; and challenging switchable divergent synthesis. On account of this, based on our ongoing interest in the exploration of practical asymmetric organocatalysis, we envisioned to solve the above two core scientific problems through using hydroxyl group as medium. We found that hydroxyl group could not only greatly enhance the activity of catalyst and substrate, but also achieve switchable divergent synthesis. Therefore, we would like to further “explore the application of hydroxy group in organocatalysis” in this project. The proposal will focus on the following topics: (1) design and synthesize new bifunctional catalysts with hydroxyl group to explore their application value; (2) activate conventional inactive sites and achieve switchable regiodivergent synthesis through introduce hydroxyl group into indoles and heterocyclic compounds; (3) explore activating effect of hydroxyl group and other substituent on inert substrates. These explorations will observably promote the vigorous development and application on organocatalysis.