Direct synthesis of arylboronic pinacol esters from arylamines

Abstract

A metal-free synthetic method for arylboronic pinacol esters from easily available aromatic amines as starting materials has been described. This novel transformation affords borylation products in good yields under mild reaction conditions. This strategy can be easily carried out in gram-scale, demonstrating the practical usefulness of the method. Moreover, the Sandmeyer-type transformation can be followed by the Suzuki–Miyaura cross-coupling reaction without purification of the arylboronate products.