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Preparation of 2‑Amino-3-arylindoles via Pd-Catalyzed Coupling between 3‑Diazoindolin-2-imines and Arylboronic Acids as well as Their Extension to 3‑Aryl-3-fluoroindolin-2-imines

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posted on 22.08.2017, 20:18 by Hualong Ding, Songlin Bai, Ping Lu, Yanguang Wang
2-Amino-3-arylindoles were conveniently prepared from 3-diazoindolin-2-imines and arylboronic acids through palladium carbene intermediates in moderate to excellent yields. The synthesized 2-amino-3-arylindoles could be fluorinated with NFSI to afford 3-aryl-3-fluoroindolin-2-imines.