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Fast continuous alcohol amination employing a hydrogen borrowing protocol

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Abstract

A continuous flow method for the direct conversion of alcohols to amines via a hydrogen borrowing approach is reported. The method utilises a low loading (0.5%) of a commercial catalyst system ([Ru(p-cymene)Cl2]2 and DPEPhos), reagent grade solvent and is selective for primary alcohols. Successful methylation of amines using methanol and the direct dimethylamination of alcohols using commercial dimethylamine solution are reported. The synthesis of two pharmaceutical agents Piribedil (5) and Buspirone (25) were accomplished in good yields employing these new methods.

Graphical abstract: Fast continuous alcohol amination employing a hydrogen borrowing protocol

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Publication details

The article was received on 23 Oct 2018, accepted on 12 Nov 2018 and first published on 16 Nov 2018


Article type: Communication
DOI: 10.1039/C8GC03328E
Citation: Green Chem., 2019, Advance Article
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    Fast continuous alcohol amination employing a hydrogen borrowing protocol

    R. Labes, C. Mateos, C. Battilocchio, Y. Chen, P. Dingwall, G. R. Cumming, J. A. Rincón, M. J. Nieves-Remacha and S. V. Ley, Green Chem., 2019, Advance Article , DOI: 10.1039/C8GC03328E

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