Synthesis of N ‐Glycosyl Conjugates through a Multicomponent Domino Process

The development of efficient methods for the combinatorial synthesis of N ‐glycosyl conjugates is vital for many fields of modern synthetic organic chemistry. Herein, we report a multicomponent domino process for the regioselective synthesis of a large array N ‐glycosyl‐Asp‐urea conjugates, which could be further functionalized in a chemoselective way, starting from easily accessible reactants such as N ‐glycosylamines, fumaric acid monoesters, azides, and isocyanates. The process occurs under very mild conditions, does not require the use of strong bases/acids or high temperature, and is highly versatile, working efficiently with a range of protecting groups and substituents.