Transition-metal-free highly regioselective C-H acetoxylation of pyrrolo[2,3-d]pyrimidine derivatives

A simple and efficient methodology was developed for the direct C(sp2)–H acetoxylation of pyrrolo[2,3-d]pyrimidine derivatives. This highly regioselective one-pot acetoxylation was carried out under transition-metal-free conditions in the presence of NaI. This protocol provides a variety of acetoxylated pyrrolo[2,3-d]pyrimidines in good to excellent yields, which are potentially of great importance in medicinal chemistry. And this methodology was also proved to be practical by the gram-scale synthesis.