A highly efficient procedure for 3-sulfenylation of indole-2-carboxylates

Org Lett. 2004 Mar 4;6(5):819-21. doi: 10.1021/ol049956v.

Abstract

A highly efficient one-pot procedure for 3-sulfenylation of 2-carboxyindoles is described. Treatment of thiols with N-chlorosuccinimide at -78 degrees C in CH(2)Cl(2) affords sulfenyl chlorides in situ that readily react with 2-carboxyindoles to give 3-thioindoles in high yields. This new method is milder, produces less waste, and is compatible with a wide range of thiol and indole functionality. [reaction: see text]