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Issue 1, 2019
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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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Supplementary files

Article information


Submitted
23 Oct 2018
Accepted
12 Nov 2018
First published
16 Nov 2018

Green Chem., 2019,21, 59-63
Article type
Communication

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, 21, 59
DOI: 10.1039/C8GC03328E

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