Fast continuous alcohol amination employing a hydrogen borrowing protocol

Ricardo Labes, Carlos Mateos, Claudio Battilocchio, Yiding Chen, Paul Dingwall, Graham R. Cumming, Juan A. Rincón, Maria José Nieves-Remacha, Steven V. Ley

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11 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)59-63
Number of pages5
JournalGreen Chemistry
Volume21
Issue number1
Early online date16 Nov 2018
DOIs
Publication statusEarly online date - 16 Nov 2018

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Labes, R., Mateos, C., Battilocchio, C., Chen, Y., Dingwall, P., Cumming, G. R., Rincón, J. A., Nieves-Remacha, M. J., & Ley, S. V. (2018). Fast continuous alcohol amination employing a hydrogen borrowing protocol. Green Chemistry, 21(1), 59-63. https://doi.org/10.1039/C8GC03328E