Improved and Highly Versatile Synthesis of 5‐Aryltropones

Abstract

The use of 5‐iodo‐2‐methoxytropone in palladium(0)‐catalyzed coupling reactions with a variety of arylboronic acids has resulted in significantly improved reaction yields and times for a sterically and electronically diverse series of novel 5‐aryltropones. In addition, the required 5‐iodo‐2‐methoxytropone was conveniently synthesized in excellent yield.

Keywords:

• Antimitotic
• arylboronic acids
• aryltropones
• colchicinoids
• palladium coupling

Acknowledgment

We thank Susan Bane of Binghamton University for her helpful discussions and advice during the course of this work and in the preparation of this paper.