有机催化不对称aza-Henry反应研究进展

Research Advances in Organocatalytic Asymmetric Aza-Henry Reaction

不对称aza-Henry反应是重要的碳碳键形成反应,手性产物β-硝基胺是许多药物和天然产物的关键中间体,利用该反应构建手性化合物已有广泛报道,其中有机催化不对称aza-Henry反应已成为不对称催化领域的重要研究对象。催化不对称aza-Henry反应的有机小分子催化剂主要有硫脲类催化剂和相转移催化剂,其中硫脲类催化剂占主要部分,其次还有方酰胺类、胍酰胺类以及脲类等催化剂。对近5年有机催化不对称aza-Henry反应的发展现状进行概述并作出总结与展望,以期为今后有机催化不对称合成研究提供参考。

Asymmetric aza-Henry reaction is an important carbon-carbon coupling reaction,and the chiral productβ-nitroamine is a key intermediate for many drugs and natural products.The construction of chiral compounds by this reaction has been widely reported.Among them,the organocatalytic asymmetric aza-Henry reaction has become important research subject in the field of asymmetric catalysis.The organic small molecule catalysts for asymmetric aza-Henry reaction mainly include thiourea catalysts and phase transfer catalysts.Among them,thiourea catalysts account for the main part,followed by squaramide,guanidine amide and urea catalysts.In this review paper,the development status of asymmetric aza-Henry reactions catalyzed by organocatalysts in the past five years was summarized and prospected to provide guidance for future researches relating organocatalytic asymmetric synthesis.