Issue 7, 2019

Robust Buchwald–Hartwig amination enabled by ball-milling

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

Supplementary files

Article information

Article type
Communication
Submitted
24 iyl 2018
Accepted
03 sen 2018
First published
18 sen 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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