A general method for the synthesis of 2,3-disubstituted indoles is described. The key feature of this method is amination of aromatic C-H bonds via FeCl2-catalyzed ring opening of 2H-azirines. The method tolerates a variety of functional groups such as Br, F, NO2, OMe, CF3, OTBS, alkenes, and OPiv. The method can be also extended to synthesize azaindoles.
Fe(II)-Catalyzed Amination of Aromatic C-H Bonds via Ring Opening of 2H-Azirines: Synthesis of 2,3-Disubstituted Indoles. -The method tolerates a broad spectrum of functionalities and can also be used for the preparation of azaindoles such as (IV). -(JANA, S.; CLEMENTS, M. D.; SHARP, B. K.; ZHENG*, N.; Org.
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