2453-91-0Relevant articles and documents
Direct Amidation of Esters by Ball Milling**
Barreteau, Fabien,Battilocchio, Claudio,Browne, Duncan L.,Godineau, Edouard,Leitch, Jamie A.,Nicholson, William I.,Payne, Riley,Priestley, Ian
, p. 21868 - 21874 (2021)
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.
Clavulanic acid biosynthesis; the final steps
Fulston,Davison,Elson,Nicholson,Tyler,Woroniecki
, p. 1122 - 1130 (2007/10/03)
The chemically unstable anabolite (3R,5R)-clavulanate-9-aldehyde 1 and an NADPH dependent dehydrogenase have been detected in the broth of Streptomyces clavuligerus. The purified enzyme was shown to make clavulanic acid by reduction of the aldehydic moiet