Pd-catalyzed Site-selective direct arene C [sbnd] H arylation of Pyrrolo[2,3-d]pyrimidine derivatives with aryl iodides

Abstract

A simple and efficient methodology was developed for the direct ortho C H arylation of pyrrolo[2,3-d]pyrimidine derivatives. Aryl iodides are chosen as an arylating reagent for C(sp2)−H bond under Pd(II)/Pd(IV) catalysis in the presence of TFA, affording a diverse array of (hetero)biaryls-containing pyrrolo[2,3-d]pyrimidines in moderate to good yields with high regioselectivity and chemoselectivity.