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The solution phase synthesis of a 150 member library of 2 aminopyrimidinones and their 6 aza analogs is described. The key intermediates for library generation, S methylpyrimidinones and S methyl 6 aza pyrimidinones, were easily prepared using typical procedures, and subsequent nucleophilic aromatic substitu tion with various amines was carried out under standardized conditions with high yields.