A highly efficient procedure for 3-sulfenylation of indole-2-carboxylates.
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]
Department of Chemistry, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
Kevin M
KM
Schlosser
Alexei P
AP
Krasutsky
Harriet W
HW
Hamilton
Jessica E
JE
Reed
Karen
K
Sexton