Robust Buchwald-Hartwig amination enabled by ball-milling

Org Biomol Chem. 2019 Feb 13;17(7):1722-1726. doi: 10.1039/c8ob01781f.

Abstract

An operationally simple mechanochemical method for the Pd catalysed Buchwald-Hartwig amination of arylhalides with secondary amines has been developed using a Pd PEPPSI catalyst system. The system is demonstrated on 30 substrates and applied in the context of a target synthesis. Furthermore, the performance of the reaction under aerobic conditions has been probed under traditional solution and mechanochemical conditions, the observations are discussed herein.

Publication types

  • Research Support, Non-U.S. Gov't