Rapid access to azetidines via allylation of azabicyclo[1.1.0]butanes by dual copper/photoredox catalysis

Abstract

Recently, the strain-release-driven synthesis of N₁/C₃ functionalized azetidines from azabicyclo[1.1.0]butanes has generated significant interest in the fields of medicinal and synthetic chemistry. This paper presents a mild and efficient dual copper/photoredox-catalyzed multi-component allylation of azabicyclo[1.1.0]butanes using a radical-relay strategy. This strategy enables the synthesis of C3 quaternary center-containing azetidines via a radical relay mechanism with a high yield of 91%. The method's utility is highlighted by late-stage derivatization of bioactive molecules, demonstrating exceptional functional group compatibility.