Nicholson, WI;
Barreteau, F;
Leitch, JA;
Payne, R;
Priestley, I;
Godineau, E;
Battilocchio, C;
(2021)
Direct Amidation of Esters via Ball Milling.
Angewandte Chemie
, 133
(40)
pp. 22039-22045.
10.1002/ange.202106412.
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Abstract
The direct mechanochemical amidation of esters by ball milling is described. The operationally simple procedure requires an ester, an amine, and substoichiometric KOtBu and was used to prepare a large and diverse library of 78 amide structures with modest to excellent efficiency. Heteroaromatic and heterocyclic components are specifically shown to be amenable to this mechanochemical protocol. This direct synthesis platform has been applied to the synthesis of active pharmaceutical ingredients (APIs) and agrochemicals as well as the gram-scale synthesis of an active pharmaceutical, all in the absence of a reaction solvent.
| Type: | Article |
|---|---|
| Title: | Direct Amidation of Esters via Ball Milling |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1002/ange.202106412 |
| Publisher version: | https://doi.org/10.1002/ange.202106412 |
| Language: | German |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry |
| URI: | https://discovery-pp.ucl.ac.uk/id/eprint/10132215 |
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