Nicholson, William I.; Barreteau, Fabien; Leitch, Jamie A.; Payne, Riley; Priestley, Ian; Godineau, Edouard; Battilocchio, Claudio; Browne, Duncan L. published the artcile< Direct Amidation of Esters by Ball Milling>, Quality Control of 93-60-7, the main research area is amide preparation ball milling; amine ester mechanochem amidation; ester amine hydrochloride mechanochem amidation; amidation; amides; ball milling; esters; sustainable chemistry.
The direct mechanochem. amidation of esters RC(O)OR1 (R = Cy, Ph, pyridin-2-yl, etc.; R1 = Me, Et) by ball milling is described. The operationally simple procedure requires an ester, amines R2NHR3 (R2 = H, Me, Et; R3 = i-Pr, Ph, 2,4,6-trimethylphenyl, etc.; R2R3 = -(CH2)2O(CH2)2-, -(CH2)5-, -(CH2)6-, etc.) and 1,2,3,4-tetrahydroquinoline, and substoichiometric KOtBu, and was used to prepare a large and diverse library of 78 amide structures RC(O)N(R2)R3 and (3,4-dihydroquinolin-1(2H)-yl)(phenyl)methanone with modest to excellent efficiency. Heteroaromatic and heterocyclic components are specifically shown to be amenable to this mechanochem. protocol. This direct synthesis platform has been applied to the synthesis of active pharmaceutical ingredients (APIs) and agrochems. as well as the gram-scale synthesis of an active pharmaceutical, all in the absence of a reaction solvent.
Angewandte Chemie, International Edition published new progress about Amidation. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Quality Control of 93-60-7.