Transition-metal-free lactamization of C(sp3)–H bonds with CO2: facile generation of pyrido[1,2-a]pyrimidin-4-ones

Abstract

A novel carbonylation of C(sp³)–H bonds in pyridylamines with one atmosphere of CO₂ is reported to synthesize important pyrimidinones in good yields. This transition-metal-free and redox-neutral process features the use of a nontoxic carbonyl source, broad substrate scope, good functional group tolerance, facile scalability and easy product derivatization.