Fast continuous alcohol amination employing a hydrogen borrowing protocol

Autor: Steven V. Ley, María José Nieves-Remacha, Claudio Battilocchio, Graham R. Cumming, Ricardo Labes, Paul Dingwall, Juan A. Rincón, Carlos Mateos, Yiding Chen
Přispěvatelé: Labes, Ricardo [0000-0003-4001-0775], Battilocchio, Claudio [0000-0002-4601-8527], Chen, Yiding [0000-0001-6932-9005], Dingwall, Paul [0000-0002-6961-7995], Ley, Steven [0000-0002-7816-0042], Apollo - University of Cambridge Repository
Rok vydání: 2018
Předmět:
DOI: 10.17863/cam.34164
Popis: 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.
Databáze: OpenAIRE