Synthesis of 2,4-diarylated pyrimidines enabled by Ni-catalyzed C–sulfone bond activation†

Herein, we report the use of the readily available and bench-stable pyrimidinyl sulfones as electrophiles in Ni-catalyzed Suzuki−Miyaura cross-coupling reactions. This method allows the facile synthesis of 2,4-disubstituted pyrimidines that are pharmaceutically relevant. These reactions were carried out under mild conditions and show a remarkable substrate scope. In this approach, the C–sulfone bond is cleaved efficiently and regioselectively. Preliminary mechanistic studies revealed the importance of the α-nitrogen atom in pyrimidine in facilitating these transformations.