氮杂环卡宾催化的α-羰基羧酸盐不对称新反应研究

Asymmetric catalysis should be the best efficient method for synthesis of chiral compounds, which could accord with demand for green chemistry. N-Heterocyclic Carbene (NHC) which is one of the most important organocatalysts, is wildly used in organic synthesis, especially in asymmetric catalysis. Aldehydes are relatively unstable, For example, some of them could be easily oxidized by air and have low boiling points. These drawbacks could hinder development and utilization in NHC-catalyzed reaction. This project wants to develop NHC catalyzed asymmetric reactions of α-keto carboxylic salts in order to solve these above problems. Furthermore, this project wants to develop a new type of reactions and which could be applied to prepare drug molecules, such as Ezetimibe and Sitagliptin. We hope this ongoing study will provide new methodologies which would be an important development and complement for the NHC catalysis，it is also very important and useful for developing and application novel reactions in the future.

不对称催化符合绿色化学的发展要求，是合成手性化合物的最有效方法。氮杂环卡宾（NHC）作为最重要的有机小分子催化剂之一，被广泛应用于有机合成中，尤其是不对称催化领域。然而底物醛的相对不稳定（如一些醛易被空气氧化，沸点低）限制了它们在NHC催化反应中的发展和应用。本项目拟通过使用α-羰基羧酸盐代替醛克服以上缺点，实现NHC催化的高效不对称反应，并将其应用到药物分子（依泽麦布和西他列汀）的合成中。该项目的顺利实施，将建立新的方法学，丰富并拓展NHC催化反应研究，为未来新反应的设计以及应用提供新途径和理论依据。

氮杂环卡宾是一类非常重要的有机小分子催化剂，被广泛用于不对称催化领域。本项目致力于发展NHC催化的新型底物和新型不对称催化反应。在NHC催化下，稳定、易得的α-羰基羧酸盐在与烯酮、靛红、1,3-二羰基化合物、2-亚乙基-1,3-茚满二酮以及亚胺等不对称反应中表现出优异的反应活性和立体选择性。随后进一步开展了NHC催化的亚胺及亚胺正离子的极性翻转等方面的研究工作。这些研究成果丰富并拓展了NHC催化，为未来新反应的设计以及应用提供新途径和理论依据。