Oxone‐Mediated Oxidative 3‐Arylthio Substitution of Indoles

Abstract

Oxone‐mediated oxidative 3‐arylthio substitution of indoles with benzenethiols in methanol has been succeeded, giving 3‐arylthioindoles. Indoles bearing a 2‐methyl group particularly exhibited higher activities toward 3‐arylthio substitutions. 3‐(2′‐Pyridylthio)indoles used as selective COX‐2 inhibitors were prepared in good to excellent yields.

Keywords:

• 3‐Arylthioindole
• benzenethiol
• 2‐mercaptopyridine
• oxone
• selective COX‐2 inhibitor

Acknowledgment

We acknowledge the financial Support of the National Natural Science Foundation of China (Project 20572040).