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

J Org Chem. 2024 Nov 1;89(21):15990-15994. doi: 10.1021/acs.joc.4c01357. Epub 2024 Oct 18.

Abstract

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%.