Direct Amidation of Esters by Ball Milling*

Autor:	William I. Nicholson, Ian Priestley, Claudio Battilocchio, Duncan L. Browne, Jamie A. Leitch, Riley Payne, Fabien Barreteau, Edouard Godineau
Rok vydání:	2021
Předmět:	Active ingredient Green chemistry Solvent chemistry.chemical_compound Chemistry Amide Mechanochemistry Amine gas treating General Medicine General Chemistry Combinatorial chemistry Ball mill Catalysis
Zdroj:	Angewandte Chemie (International ed. in English). 60(40)
ISSN:	1521-3773
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a90b8464b55266f578851bbd4bcbf51a https://pubmed.ncbi.nlm.nih.gov/34357668 Zobrazit plný text záznamu Plný text