3-Sulfenylation of indole-2-carboxylates

摘要

A highly efficient one-pot procedure for 3-sulfenilation of indole 2-carboxylates is described. Treatment of thiols with N-chlorosuccinimide at -78° C. in CH2Cl2 affords sulfenyl chlorides in situ that readily react with indole 2-carboxylates 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.