Solid phase synthesis of 5,6-disubstituted pyrimidinone and pyrimidindione derivatives

Solid phase synthesis of 5,6-disubstituted pyrimidinone and pyrimidindione derivs., e.g. I and II, were prepd., in 88 and 85% yield, by condensing polymer bound thiouronium salts with β-ketoesters, e.g. Et acetoacetate, and cleavage of the product with TFA and Oxone/H2O/dioxane, resp. Combinatorial libraries of pyrimidindiones, 2-thiopyrimidinones, and 2-methoxypyrimidinones were generated by using a Syncore Reactor. Solid phase synthesis of 5,6-disubstituted pyrimidinone and pyrimidindione derivatives by the use of the Syncore® Reactor is described starting from easily available building blocks.