Cs2CO3 catalyzed direct aza-Michael addition of azoles to α,β-unsaturated malonates

Abstract

A highly efficient method for the synthesis of azole derivatives via a direct aza-Michael addition of azoles to α,β-unsaturated malonates using Cs₂CO₃ as a catalyst, has been successfully developed. A series of azole derivatives have been obtained in up to 94% yield and the reaction could be amplified to gram scale in excellent yield in the presence of 10 mol% of Cs₂CO₃.