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Robust Buchwald–Hartwig amination enabled by ball-milling†
Qun Cao,William I. Nicholson,Andrew C. Jones,Duncan L. Browne
Organic & Biomolecular Chemistry Pub Date : 09/18/2018 00:00:00 , 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.

Graphical abstract: Robust Buchwald–Hartwig amination enabled by ball-milling
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