An efficient soluble polymer-supported method has been developed for the parallel synthesis of substituted benzimidazole linked benzoxazoles using focused microwave irradiation. The key step involves the amidation of 4-hydroxy-3-nitrobenzoic acid with polymer-immobilized o-phenylenediamine. Application of mild acidic conditions promoted the ring closure to furnish the benzimidazole ring. After ...

An efficient copper-catalyzed direct 2-arylation of benzoxazoles and benzoimidazoles with aryl bromides is presented. The CuI/PPh3-based catalyst promotes the installation of various aryl and heteroaryl groups through a C-H activation process in good to excellent yields. The cytotoxicity of obtained 2-aryl benzoxazoles (benzoimidazoles) was also evaluated and 1-methyl-2-(naphthalen-1-yl)benzoim...

Synthesis and antimicrobial activity of new metal [Mg(II), Fe(II), Co(II), Ni(II), Zn(II) and Cd(II)] complexes from 2-(1’/2’-hydroxynaphthyl)benzoxazoles have been described. Some of the metal complexes show significant antifungal activity (MIC <3.12 μg/ml). Further, 2-(1’/2’hydroxynaphthyl)benzoxazoles exhibit excited-state intramolecular proton transfer mechanism that has been studied using ...

In this study, zirconium dodecylphosphonate was synthesized by the reported method in scientific literature. 2-Alkylbenzoxazoles were prepared from aliphatic carboxylic acids and 2-aminophenol in the presence of this catalyst under solvent-free conditions at 100°C. Their structures were recognized by IR, 1H NMR, and 13C NMR. Then, we used aromatic carboxylic acids in t...

A wide range of 2-substituted benzoxazoles can be efficiently synthesized from N-(2-iodo-/bromo-phenyl)benzamides, and even the less reactive N-(2-chlorophenyl)benzamides, via Cu-catalysed intramolecular coupling cyclization reactions using methyl 2-methoxybenzoate as the ligand under mild reaction conditions. In addition, the benzoxazoles can be easily prepared from the primary amides coupling...

A series of 2-(p-substituted-benzyl)-5-[[4-(p-chloro/fluoro-phenyl)piperazin-1-yl]acetamido]-benzoxazoles were synthesized in need of new compounds for the fight against microbial pathogens. Their structures were elucidated by spectral techniques. These new derivatives, along with previously synthesized 2-(p-substituted-benzyl)-5-substituted-benzoxazoles, were evaluated for their antibacterial ...

A series of 2-(p-substituted phenyl)-5-(2-{4-[(p-chloro-fluorophenyl)/phenyl] piperazin-1-yl}acetamido)-benzoxazoles were synthesized and tested for their antimicrobial activities. The structures of the new derivatives were elucidated by spectral techniques. The minimum inhibitory concentrations (MIC) of the new benzoxazoles, along with those of previously synthesized analogues, were determined...

To design new compounds suitable as starting points for anticancer drug development, we have synthesized a novel series of benzoxazoles with pharmaceutically advantageous piperazine and fluorine moieties attached to them. The newly synthesized benzoxazoles and their corresponding precursors were evaluated for cytotoxicity on human A-549 lung carcinoma cells and non-cancer HepaRG hepatocyes. Som...

The first example of DAST-promoted Beckmann rearrangement/intramolecular cyclization of acyclic ketoximes is described. This unique protocol represents a direct and effective pathway to 2-oxazolines, benzimidazoles and benzoxazoles in moderate to good yields.

Ten new 2-(3-aryl-1-phenyl-4-pyrazolyl)benzoxazoles have been synthesized by oxidative intramolecular cyclization of the corresponding Schiff's bases using iodobenzene diacetate in methanol as an oxidant.