Divergent solution-phase synthesis of diarylpyrimidine libraries as selective A3 adenosine receptor antagonists.

A practical and divergent solution-phase synthetic strategy has been optimized to prepare a highly diverse library of 2,4-diaryl- and 2,6-diarylpyrimidines. Structural elaboration of the starting heterocyclic scaffolds was accomplished by exploiting the potential for diversity offered by the Suzuki−Miyaura cross-coupling reaction. These studies enabled the identification of structurally simple, highly potent, and selective A3 adenosine receptor antagonists.