Palladium-catalyzed selective N-(hetero)arylation or N,N′-di(hetero)arylation of 1-aminoindoles

Messaoudi, Samir; Brion, Jean-Daniel; Alami, Mouâd

Palladium-catalyzed selective N-(hetero)arylation or N,N′-di(hetero)arylation of 1-aminoindoles

2011

Messaoudi, Samir | Brion, Jean-Daniel | Alami, Mouâd

The selective synthesis of N-(hetero)aryl-1-aminoindoles 3 from the corresponding N-aminoindoles and (hetero)aryl halides using a catalyst combination of Pd₂(dba)₃ associated to Josiphos is described. By switching to Xantphos as the ligand, the alternate catalytic system allows the coupling to proceed efficiently for the preparation of symmetrical and unsymmetrical N,N′-diaryl-1-aminoindole derivatives in good yields.

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