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Direct amidation of esters by ball milling**

Nicholson, William I., Barreteau, Fabien, Leitch, Jamie A., Payne, Riley, Priestley, Ian, Godineau, Edouard, Battilocchio, Claudio and Browne, Duncan L. ORCID: 2021. Direct amidation of esters by ball milling**. Angewandte Chemie International Edition 60 (40) , pp. 21868-21874. 10.1002/anie.202106412

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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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Publisher: Wiley
ISSN: 1433-7851
Last Modified: 11 Mar 2023 02:53

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