An Easy Access to Pyrogallol Derivatives Using a Practical Auxiliary

Abstract

This paper describes a facile approach topyrogallol derivativesvia a palladium-catalyzed bis-CÀ H acetoxylation strategy with 5-nitropyrimidine as a directing group (DG). The directing group can be easily pre-installed and readily removed under mild condition after the coupling. In addition, the transformation is operationally simple, has high functional group tolerance, and is amenable to gram-scale. Moreover, the 5nitropyrimidine is successfully used as a practical directing group that three-step installation of directing group, orthoacetoxylation and removalof the directing group sequence were successfullycombined in one pot.