Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry at Fuzhou University, Fuzhou, Fujian, 350108, China.
Nat Commun. 2021 Jan 19;12(1):441. doi: 10.1038/s41467-020-20727-7.
Multicomponent reactions (MCRs) facilitate the rapid and diverse construction of molecular scaffolds with modularity and step economy. In this work, engagement of boronic acids as carbon nucleophiles culminates in a Passerini-type three-component coupling reaction towards the synthesis of an expanded inventory of α-hydroxyketones with skeletal diversity. In addition to the appealing features of MCRs, this protocol portrays good functional group tolerance, broad substrate scope under mild conditions and operational simplicity. The utility of this chemistry is further demonstrated by amenable modifications of bioactive products and pharmaceuticals as well as in the functionalization of products to useful compounds.
多组分反应（MCRs）促进了分子支架的快速和多样化构建，具有模块化和经济性。在这项工作中，硼酸作为碳亲核试剂的参与导致了 Passerini 型三组分偶联反应，从而合成了具有骨架多样性的扩展的α-羟基酮库。除了 MCRs 的吸引人的特点外，该方案还表现出良好的官能团耐受性、在温和条件下的广泛底物范围和操作简单性。通过对生物活性产物和药物的可修饰性以及对有用化合物的产品功能化，进一步证明了这种化学的实用性。
