Solid-phase rhodium carbenoid N-H insertion reactions: the synthesis of a diverse array of indoles

J Comb Chem. 2003 Mar-Apr;5(2):188-96. doi: 10.1021/cc020079z.

Abstract

A solid-phase synthesis of an array of indoles is reported. The key step in our approach involves a N-H insertion reaction of N-alkylanilines into a highly reactive polymer-bound rhodium carbenoid intermediate to yield the corresponding alpha-arylamino-beta-ketoester. These insertion products were then treated under acid-catalyzed cyclodehydration conditions to yield a series of polymer-bound indole esters, which were subsequently cleaved from the resin under Lewis acid-promoted amidation conditions to yield the desired indoles in good yields and with excellent purities.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Catalysis
  • Cyclization
  • Indicators and Reagents
  • Indoles / chemical synthesis*
  • Resins, Synthetic
  • Rhodium / chemistry*

Substances

  • Indicators and Reagents
  • Indoles
  • Resins, Synthetic
  • Rhodium