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Robust Buchwald–Hartwig amination enabled by ball-milling

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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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Publication details

The article was received on 24 Jul 2018, accepted on 03 Sep 2018 and first published on 18 Sep 2018


Article type: Communication
DOI: 10.1039/C8OB01781F
Citation: Org. Biomol. Chem., 2018, Advance Article
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    Robust Buchwald–Hartwig amination enabled by ball-milling

    Q. Cao, W. I. Nicholson, A. C. Jones and D. L. Browne, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C8OB01781F

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