An efficient synthesis of 1,3-disubstituted 5-diethoxyphosphoryluracils

Abstract An efficient three-step procedure for the synthesis of 1,3-disubstituted 5-diethoxyphosphoryluracils is presented. The starting 2-diethoxyphosphorylacetamides were subjected to dimethylaminomethylidenation using N , N -dimethylformamide-dimethyl acetal and the 3-dimethylamino-2-diethoxyphosphorylpropenamides obtained were transformed into N , N ′-disubstituted 3-amino-2-diethoxyphosphorylpropenamides by treatment with various amines. Cyclization in the presence of phosgene led to an efficient formation of the title compounds.