Development of a Divergent Synthesis Strategy for 5-Sulfonyl-Substituted Uracil Derivatives

An efficient, diversity-orientated synthesis of 5-sulfone-substituted uracils was established. The use of protecting groups to synthesize sulfones from N-heterocycles was avoided. Various heterocycles were synthesized for the first time from favorable, easily accessible starting materials. Diversity-orientated syntheses are important for the medicinal chemistry of virostatics and chemotherapeutics. This approach provides a broad substrate tolerance and excellent yields of up to 98%.