Synthesis of 1,4,5 trisubstituted γ-lactams via a 3-component cascade reaction

Abstract

A three component one-pot cascade reaction was developed for the synthesis of 1,4,5-trisubstituted γ-lactams. The resulting scaffold can be modified independently at three positions, two of which are conveniently accessed by changing the components of the one-pot reaction. The phases of building block generation, scaffold synthesis and subsequent appendage modification were adapted to library production, which resulted in a screening library of 500 compounds.

Keywords: Cascade reaction; Library production; Molecular diversity; One-pot reaction; γ-Lactams.