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.

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