Z Zhang, Zhipeng Zhan, Bin Liu, Jiaqi Tong, C B Li, Xi Zhang
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.