Ambient-Light-Promoted Three-Component Annulation: Synthesis of Perfluoroalkylated Pyrimidines

An ambient-light-promoted and metal-free three-component reaction of active methylene compounds, perfluoroalkyl iodides, and guanidines/amidines is reported. This constitutes a powerful method to prepare perfluoroalkylated pyrimidines with mild reaction conditions, broad substrate scope, excellent functional group tolerance, and simple operation. A radical/polar mechanism involving the formation of a halogen-bond adduct and radical cross-coupling is proposed.本研究报道了一种环境光促进、无金属参与的活性亚甲基化合物、全氟烷基碘化物与胍/脒类化合物的三组分反应。该方法为制备全氟烷基化嘧啶类化合物提供了一条高效合成路径，具有反应条件温和、底物适用范围广、官能团兼容性优异且操作简便的优势。本研究提出了一种涉及卤键加合物生成与自由基交叉偶联的自由基-极性交叉反应机理。