Pd-Catalyzed highly selective and direct ortho C–H arylation of pyrrolo[2,3-d]pyrimidine derivatives

Abstract

The first Pd-catalyzed one-pot direct ortho C–H arylation of pyrrolo[2,3-d]pyrimidine derivatives is reported. Many functional groups are well tolerated under these direct C–H arylation conditions. This protocol provides a variety of biphenyl-containing pyrrolo[2,3-d]pyrimidines in good to excellent yields, which are potentially of great importance in medicinal chemistry. Diarylation and heteroarylation were both demonstrated to be effective and this methodology was also proved practical for gram-scale synthesis.