One-pot construction of functionalized aziridines and maleimides via a novel pseudo-Knoevenagel cascade reaction
An Ugi, novel pseudo-Knoevenagel, ring expansion cascade reaction was discovered and utilized for the synthesis of aziridinyl succinimides in one-pot. Subsequently, densely functionalized aziridines and maleimides have been designed and synthesized through the similar cascade reactions. The targeted compounds were prepared by means of the mild reaction and simple operation procedure, which could be applicable to a broad scope of starting materials. This series of novel cascade reactions generates opportunities for the tailored synthesis of a wide range of biologically active scaffolds through tuneable Ugi inputs. Discovery of compound 8i with comparable potency to sorafenib in the liver cancer cell lines could provide a new avenue for the liver cancer drug discovery.