Rhodium(II/III)-Catalyzed P(III)-Directed ortho C–H Diarylation/Monoalkylation of 7-Aryl-pyrrolo[2,3- d ]pyrimidine Derivatives

Rh-catalyzed, P(III)-directed arene ortho C-H diarylation and monoalkylation reactions of 7-aryl-pyrrolo[2,3-d]pyrimidine derivatives have been developed. A series of structurally diverse diarylated and monoalkylated phosphoryl-substituted pyrrolo[2,3-d]pyrimidine derivatives were obtained in moderate to good yields. The broad substrate scopes, good functional group tolerance, and high site selectivity render this strategy well-suited for the late-stage structural modification of pyrrolo[2,3-d]pyrimidine-based natural products and pharmaceuticals. This protocol enriches the library of biologically privileged pyrrolo[2,3-d]pyrimidine derivatives for further pharmacological evaluation.