Temperature-Controlled Synthesis of Thiophenol-VBXs from EBXs and Thiophenols

Abstract

Vinylbenziodoxolones (VBXs) are important electrophilic alkene synthons. However, the synthesis of cis-thiophenol-VBX reagents from ethynylbenziodoxolones (EBXs) and thiophenols remains challenging. Herein, we explore an efficient method for the synthesis of cis-thiophenol-VBXs in excellent yield with excellent regio- and stereoselectivities from EBXs and thiophenols under temperature-controlled conditions.