Synthesis of 4-functionalized-1H-indoles from 2,3-dihalophenols†
Roberto Sanz,Verónica Guilarte,Nuria García
Organic & Biomolecular Chemistry Pub Date : 07/08/2010 00:00:00 , DOI:10.1039/C004360E
Abstract

A new synthesis of 4-halo-1H-indoles has been developed from easily available 2,3-dihalophenol derivatives. The key steps are Smiles rearrangement and a one-pot or stepwise Sonogashira coupling/NaOH-mediated cyclization. Subsequent functionalization allows access to a wide variety of 2,4- or 2,3,4-regioselectively functionalized indoles.

Graphical abstract: Synthesis of 4-functionalized-1H-indoles from 2,3-dihalophenols