Approaches to the synthesis of 2,3-dihaloanilines. Useful precursors of 4-functionalized-1H-indoles.

摘要: 2,3-Dihaloanilines have been proved as useful starting materials for synthesizing 4-halo-1H-indoles. Subsequent or in situ functionalization of the prepared haloindoles allows access to a wide variety 2,4- 2,3,4-regioselectively functionalized indoles good overall yields. As no efficient synthetic routes 2,3-dihaloanilines described literature, different approaches preparation these 1,2,3-functionalized aromatic precursors are now presented. The most general one involves Smiles rearrangement from corresponding 2,3-dihalophenols and 2,3-dihaloanilides straightforward synthetically manner.