手性醛催化氨甲基化合物的直接不对称α-官能化反应

手性醛催化氨甲基化合物的直接不对称α-官能化反应是当前合成手性胺和手性氨基酸最具步骤经济性的不对称催化策略之一，但是，到目前为止仅有手性醛催化的不对称烷基化、共轭加成、烯丙基化和Mannich反应得以成功实现，并且这四例化学反应均是使用氨基酸衍生物作为亲核试剂。通过变换参与反应的氨甲基化合物和亲电试剂的种类，即有可能实现手性醛催化的多类型不对称直接α-官能化反应，这赋予了手性醛催化广阔的研究空间。此外，手性胺和手性氨基酸具有极好的市场价值，发展相应的手性醛催化新工艺路线具有不错的应用前景。本项目不仅研究手性醛催化氨基酸参与的新型不对称α-官能化反应来合成非天然手性氨基酸，还将首次研究手性醛催化芳基甲胺的不对称α-官能化反应来合成手性胺，并开发出合成具有市场价值的手性胺和手性氨基酸的手性醛催化新工艺路线。

Chiral aldehyde catalysed direct asymmetric α-functionalization of aminomethyl compounds is one of the most straightforward strategies for the preparation of chiral amines and amino acids. However, to date, there are only four reactions have been successfully realized, including the chiral aldehyde catalyzed α-alkylation, conjugated addition, α-allylation and Mannich reactions. All of these four transformations employed amino acid derivatives as the sole type of nucleophile. In principle, novel α-functionalization reactions can be achieved through introducing new types of aminomethyl compounds and electrophiles as reagents, which provides a broad research space for chiral aldehyde catalysis. In addition, chiral amine and amino acids have good commercial value. So, it is an important work to develop new technical synthetic rout leading to those target molecules by chiral aldehyde catalysis. In this project, we will focus on the creation of new α-functionalization reactions of aminomethyl compounds such as amino acids and α-aryl substituted methylamines for the preparation of chiral amino acids and amines, and the development of novel technical synthetic rout leading to commercial available chiral amino products.