SIMPLE AND EFFICIENT SYNTHESIS OF PHOSPHORYLATED THIENOPYRIDONES FROM 2-AMINOTHIOPHENE-3-CARBOXYLATES AND P-PHOSPHONYLKETONES

摘要

Herein, we report an efficient and straightforward synthesis of the new 5-phosphonothieno[2,3-b]pyridin-4(5H)-ones, via the p-toluenesulfonic acid catalyzed reaction of ethyl 2-aminothiophene-3-carboxylates with β-phosphonylketones. To the best of our knowledge, this is the first synthesis of thienopyridone derivatives bearing a phosphonate or a phosphine oxide group.