A green and highly efficient synthetic method for the synthesis of quinazoline‐2,4‐diones with hydrogen peroxide as the terminal oxidant has been developed. The reaction features the mild reaction conditions, broad substrate scope, metal‐free catalysts, and sole byproduct water. A plausible mechanism for this process was proposed. Moreover, an antibacterial activity study was performed to evaluate the antimicrobial activities towards two Gram‐negative bacterial strains (Escherichia coli, and Klebsiella pneumonia) and two Gram‐positive bacterial strains (Staphylococcus epidermidis, and Staphylococcus aureus) using the Broth microdilution method.
A convenient and metal‐free DMAP‐catalyzed domino reaction of isatins, arylamines and hydroximoyl chlorides has been developed to achieve 1,3‐dipolar cycloaddition of imines into aryl nitrile oxides at ambient temperature. In this one‐pot transformation, a 1,2,4‐oxadiazole skeleton was efficiently formed. This methodology needs no extra additives and features wide substrate scope, good functional group tolerance and mild reaction conditions. A plausible mechanism for this process was proposed. Moreover, the antibacterial activities of the products were evaluated towards Staphylococcus epidermidis, Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae using the Broth microdilution method.
Reported here is a convenient catalyst-free method for preparing a series of spiro[indoline-3,2′-pyrroles] from a three-component reaction of isatins, α-amino acid and phenylpropiolic acid esters in refluxing isopropanol with high regioselectivity and yields.
The cover picture shows a green and highly efficient synthetic method for the synthesis of quinazoline‐2,4‐diones from readily available isatins and arylamines. This method is interesting in keeping with the notion of green chemistry because of the use of hydrogen peroxide as the terminal oxidant. The rearrangement oxidation exhibited good functional group tolerability, metal‐free catalysts, obviating the need for oxidants and only environmentally benign H2O was released. Moreover, an antibacterial activity study was performed to evaluate the antimicrobial activities. The results showed that some of the testing compounds inhibited the growth of the Staphylococcus aureus (32 μg/mL) and Staphylococcus epidermidis (64 μg/mL), which could potentially solve the problem of multidrug resistance. More details are discussed in the article by Shang et al. on page 1835–1843.
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