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Fe(II)-Catalyzed Amination of Aromatic C−H Bonds via Ring Opening of 2H-Azirines: Synthesis of 2,3-Disubstituted Indoles

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journal contribution
posted on 03.09.2010, 00:00 by Samaresh Jana, Mack D. Clements, Barry K. Sharp, Nan Zheng
A general method for the synthesis of 2,3-disubstituted indoles is described. The key feature of this method is the 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 also be extended to synthesize azaindoles.

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