Ru-catalyzed direct arene C–H amidation of pyrrolo[2,3-d]pyrimidines with sulfonyl azides

[Display omitted] Ru-catalyzed direct C–H amidation of pyrrolo[2,3-d]pyrimidine derivatives was developed using sulfonyl azides as the amino source in a mild, efficient and highly chemoselective manner. The promising protocol has good compatibility with diverse functional groups and high regioselectivity, providing various structurally versatile monoamidated pyrrolo[2,3-d]pyrimidines in good to excellent yields with potential biological and therapeutic activity.