Nicholson, William I. published the artcileDirect Amidation of Esters by Ball Milling, Quality Control of 6346-09-4, the publication is Angewandte Chemie, International Edition (2021), 60(40), 21868-21874, database is CAplus and MEDLINE.
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 6346-09-4. 6346-09-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Ether, name is 4,4-Diethoxybutan-1-amine, and the molecular formula is C8H19NO2, Quality Control of 6346-09-4.
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