应用Ugi/Michael串联反应构建杂环化合物的研究进展

Progress in Synthesis of Heterocyclic Compounds by Ugi/Michael Tandem Reaction

杂环化合物是许多天然产物和药物分子的核心骨架,具有广泛的生物活性和药理作用。如何快速高效地构建小分子杂环化合物库成为当今药物化学领域的研究热点。Ugi反应在合成分子多样性方面具有得天独厚的优势,能够解决待合成化合物数量庞大、结构复杂的难题;同时Michael加成反应能快速形成C-C/C-N键,从而构建出不同骨架的环系。目前,Ugi/Michael串联反应已经成为构建杂环化合物的有力工具。作者长期致力于应用Ugi串联反应构建具有潜在药理活性的杂环分子,将近年来Ugi/Michael串联反应的研究进展与课题组的研究工作相结合对这一领域进行综述。

Heterocyclics are the core structure of many natural products and drug molecules which have a wide range of biological and pharmacological activities.So efficient construction of heterocyclic compound libraries has become one of the research hotspots in the organic synthesis field.Ugi/Michael tandem reaction has been frequently used as a powerful tool to synthesize heterocyclic compounds,because Ugi reaction has unique advantages in generating molecular diversity to gain a large quantity of products with complex properties and Michael addition reaction can be established to construct heterocyclic ring system by the formation of C-C/C-N bond.Great efforts are made by the author’ s group to apply Ugi reaction cascade in building up heterocyclic molecules with potential pharmacological activities,therefore,the recent progress in Ugi/Michael tandem reaction combined with research of our group is summarized.