Direct Amidation of Esters by Ball Milling was written by Nicholson, William I.;Barreteau, Fabien;Leitch, Jamie A.;Payne, Riley;Priestley, Ian;Godineau, Edouard;Battilocchio, Claudio;Browne, Duncan L.. And the article was included in Angewandte Chemie, International Edition in 2021.Name: Methyl benzofuran-2-carboxylate This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Name: Methyl benzofuran-2-carboxylate).
Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Name: Methyl benzofuran-2-carboxylate
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem