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. (c) 2021 Elsevier Ltd. All rights reserved.
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