One-Pot Multicomponent Mechanosynthesis of Polysubstituted trans-2,3-Dihydropyrroles and Pyrroles from Amines, Alkyne Esters, and Chalcones

An efficient and practical one-pot multicomponent reaction of amines with alkyne esters and chalcones promoted by I2/PhI­(OAc)2 has been developed under solvent-free ball-milling conditions to afford a variety of polysubstituted trans-2,3-dihydropyrroles in moderate to good yields. The present method features a short reaction time, mild reaction conditions, broad substrate scope, and feasibility of large-scale synthesis. Intriguingly, this protocol can also furnish the corresponding synthetically more attractive pyrroles with the addition of an oxidant in a one-pot way.