Efficient synthesis of 2,5-disubstituted tetrazolesvia the Cu2O-catalyzed aerobic oxidative direct cross-coupling of N–H free tetrazoles with boronic acids

Abstract

We present a new protocol that allows for the synthesis of 2,5-disubstituted tetrazolesvia the direct coupling of N–H free tetrazoles and low toxic boronic acids in the presence of only a catalytic amount of Cu₂O (5 mol%) as catalyst and 1 atm of environmentally benign O₂ as oxidant, without the need for other additives. This method represents a simple, green, and atom-efficient synthesis of 2,5-disubstituted tetrazoles.