Copper-catalyzed synthesis of cyclopropyl bis(boronates) from aryl olefins and carbon monoxide

Abstract

Cyclopropanes, especially substituted cyclopropanes, play important roles in many pharmaceuticals and in organic synthesis. In this communication, we introduced a new strategy for the synthesis of diborylated cyclopropanes via a copper-catalyzed carbonylation process. This process was successfully performed on both stable internal and terminal aryl olefins. A series of cyclopropyl bis(boronates) were produced in moderate to good yields with complete diastereoselectivity. Further synthetic transformations of the obtained cyclopropyl bis(boronates) have been accomplished to demonstrate their utility as well.