A concise approach to 2-pyrrolin-5-one scaffold construction from α-halohydroxamates and β-keto compounds.

A concise approach to the construction of the 2-pyrrolin-5-one scaffold was developed via a one-pot reaction with formal [3 + 2] annulation/elimination between β-keto nitrile/β-keto ester and unsubstituted α-halohydroxamates. This reaction features mild conditions, easy handling, broad substrate scope and good yields. Remarkably, the products could be readily converted into potentially bioactive alkylidenepyrrolinones, pyrroles, pyran-fused pyrrole heterocycles and other useful compounds, exhibiting versatile synthetic potential.