Fast Continuous Alcohol Amination Employing a Hydrogen Borrowing Protocol
Cumming, Graham R
Nieves-Remacha, Maria José
Royal Society of Chemistry (RSC)
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Labes, R., Mateos, C., Battilocchio, C., Chen, Y., Dingwall, P., Cumming, G. R., Rincón, J., et al. (2018). Fast Continuous Alcohol Amination Employing a Hydrogen Borrowing Protocol. Green Chemistry https://doi.org/10.1039/C8GC03328E
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.
Is supplemented by: https://doi.org/10.17863/CAM.31732
The authors are grateful to Eli Lilly & Co. (RL) and the EPSRC (SVL, grants EP/K009494/1, EP/M004120/1 and EP/K039520/1) for financial support. This work was supported by Eli Lilly & Co. through the Lilly Research Award Program (LRAP).
External DOI: https://doi.org/10.1039/C8GC03328E
This record's URL: https://www.repository.cam.ac.uk/handle/1810/286858