Under mild conditions, C3-quaternary 2H-pyrrolines can be convergently and efficiently assembled by Cu(II) and weak bases cocatalyzed [3+2] cycloaddition of 1,1-disubstituted alkenes and isocyanoacetates. Various functionalities can be tolerated, affording 2H-pyrrolines with up to two quaternary centers in a single step.
Keywords: 2H-pyrroline, copper catalysis, isocyanoacetate, isonitrile, cycloaddition, quaternary carbon.