Issue 7, 2019

Robust Buchwald–Hartwig amination enabled by ball-milling


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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Article information

Article type
24 Jul 2018
03 Sep 2018
First published
18 Sep 2018
This article is Open Access
Creative Commons BY license

Org. Biomol. Chem., 2019,17, 1722-1726

Robust Buchwald–Hartwig amination enabled by ball-milling

Q. Cao, W. I. Nicholson, A. C. Jones and D. L. Browne, Org. Biomol. Chem., 2019, 17, 1722 DOI: 10.1039/C8OB01781F

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