Author/Authors :
Ketcha، نويسنده , , Daniel M and Wilson *، نويسنده , , Lawrence J and Portlock، نويسنده , , David E، نويسنده ,
Abstract :
The solid-phase version of the Nenitzescu indole synthesis of 5-hydroxyindole-3-carboxamides is reported. This process involves initial acetoacetylation of ArgoPore®-Rink-NH2 resin with diketene to afford a polymer-bound acetoacetamide. Formation of the corresponding enaminones via condensation with primary amines in the presence of trimethylorthoformate followed by addition of 1,4-benzoquinones leads to the desired indoles after TFA induced cleavage from the resin.
