Synthesis and Molecular Modeling Studies of 2-[2-(3-nitrophenyl)-1h-benzimidazol-1-yl]-acetamide Derivatives as Anthelmintic

Benzimidazole derivatives of substituted 2 [2-(3-nitrophenyl)-1H-benzimidazole-1-yl] acetamide analogues were synthesized and studied for antihelminthic activity. Compounds 3a–o were obtained in three steps, starting with the Oxidative Condensation of the appropriate 3-nitrobenzaldeyde, o-phenylenediamine and sodium hydrogen sulfite to form 2-(3-nitrophenyl)-1H-benzimidazole (1a). In second step Nucleophilic substitution, Chlorine atom of ethylchloroacetate will attach on nitrogen of benzimidazole by replacing hydrogen with elimination of hydrochloric acid to form ethyl [2-(3-nitrophenyl)-1H-benzimidazole-1-Yl acetate (2a).In third step amide formation from ester takes place by substitution of electrophilic with loss of ethanol to form substituted 2 [2-(3-nitrophenyl)-1H-benzimidazole-1-yl] acetamide 3a–o The antihelminthic activity showed that compounds 3f, 3h, 3i, 3j and 3k good activity against Indian earthworms (Pheretima posthuma) in comparison to albendazole.

Chemical Oxidative Condensation of Benzidine in Non-Aqueous Medium: Synthesis and Investigation of Oligomers and Polymer with Benzidine Diimine Units

The oxidative condensation of benzidine has been carried out in acetic acid media using potassium peroxydisulfate as the oxidizing agent. Using different monomer–oxidant molar ratios, benzidine dimer, trimer, and polymer have been synthesized for the first time. It was established that the polybenzidine structure is composed from a sequence of benzidinediimine and diphenylene units with amino/amino end groups and thus proves the possibility of ammonia elimination during the oxidative polymerization of aromatic diamines. The method seems to be common for the synthesis of polymers with the sequence of aromatic diimine and arylene units. TGA analysis of the obtained trimer and polymer was investigated, and the high thermostability of both the polymer and trimer was revealed. According to the obtained data, both polymer and trimer matrix decomposition started at 300 °C, and at 600 °C, 75.94% and of 69.40% of the initial weight remained, correspondingly. Conductivities of the polymer and trimer show a semiconductor-type change from temperature and after doping show an increase in conductivity up to 10−4 Sm/cm.

Ceric Ammonium Nitrate supported on Hy-Zeolite Catalyzed Oxidative Condensation Reaction and its Docking Studies

The chemistry of chalcone has been recognized as a significant field of study. Chalcone serve as to prepare starting materials for the synthesis of various heterocyclic compounds. From the backbone of reported literature, we have developed an alternative heterogeneous and simple catalytic system for the synthesis of chalcones via the oxidative condensation of benzyl alcohol with substituted acetophenone using metal nitrate supported HY-Zeolite as a catalyst. 30 mol% CAN supported HY-zeolite has been efficiently used as a catalyst for the oxidative condensation reaction of benzyl alcohol with substituted acetophenones in the presence of hydrogen peroxide as an oxidant in toluene to afford the corresponding chalcones in good to moderate yields. Docking studies were carried out for the synthesized compounds towards the protein Lysine aminotransferase using the software.

Domino Suzuki-Miyaura Cross-Coupling and Oxidative Condensation Reaction: An Approach Towards Synthesis of Phenanthridine and Its Analogues

Phenanthridines belong to a very important class of nitrogen containing heterocylic compounds and constitute core structure of many natural alkaloids such as trisphaeridine and nitidine. Quarternarybenzo[c]phenanthridine alkaloids (QBA) represented by sanguinarine(SA), chelerythrine (CHE), and fagaronine (FA) exhibit antifungal and nematocidal properties and also serve as the core structure of broad range of medicinally active molecules showing anti-tumor activity, anti-viral property, anti-neoplastic or mutagenic activity through DNA-intercalation. Phenanthridines are also utilized for the synthesis of compounds of therapeutic interests such as anticancer platinum complex typified by phenanthriplatin antibacterial, anti-infectives, antprotozoal, antituberculosis, antitrypanosomiasis compounds. Although conventional synthetic methods towards their development showed their own advantages, they generally involved either multistep processes with low yield, or starting materials which are not readily available or requirement of prefunctionalization. Hence herein we present the development of an efficient and convenient synthetic methodology towards these versatile compounds. <br>

Domino Suzuki-Miyaura Cross-Coupling and Oxidative Condensation Reaction: An Approach Towards Synthesis of Phenanthridine and Its Analogues

Phenanthridines belong to a very important class of nitrogen containing heterocylic compounds and constitute core structure of many natural alkaloids such as trisphaeridine and nitidine. Quarternarybenzo[c]phenanthridine alkaloids (QBA) represented by sanguinarine(SA), chelerythrine (CHE), and fagaronine (FA) exhibit antifungal and nematocidal properties and also serve as the core structure of broad range of medicinally active molecules showing anti-tumor activity, anti-viral property, anti-neoplastic or mutagenic activity through DNA-intercalation. Phenanthridines are also utilized for the synthesis of compounds of therapeutic interests such as anticancer platinum complex typified by phenanthriplatin antibacterial, anti-infectives, antprotozoal, antituberculosis, antitrypanosomiasis compounds. Although conventional synthetic methods towards their development showed their own advantages, they generally involved either multistep processes with low yield, or starting materials which are not readily available or requirement of prefunctionalization. Hence herein we present the development of an efficient and convenient synthetic methodology towards these versatile compounds. <br>

Oxidative Condensation of Furfural with Ethanol Using Pd-Based Catalysts: Influence of the Support

PdO nanoparticles were deposited on several supports (β-zeolite, Al2O3, Fe2O3, MgO, and SiO2), which displayed different crystallinity, textural properties, and amount of acid and basic sites. These catalysts were characterized by X-ray diffraction (XRD), transmission electron microscopy (TEM), N2 adsorption–desorption isotherms at −196 °C, NH3 and CO2 thermoprogrammed desorption analyses (NH3- and CO2-TPD, and X-ray photoelectron spectroscopy (XPS). Pd-based catalysts were tested in the oxidative condensation of furfural with ethanol to obtain value-added chemicals. The catalytic results revealed high conversion values, although the presence of a high proportion of carbonaceous deposits, mainly in the case of the PdO supported on β-zeolite and Al2O3, is also noteworthy. The presence of basic sites led to a beneficial effect on the catalytic behavior, since the formation of carbonaceous deposits was minimized. Thus, the 2Pd-MgO (2 wt.% Pd) catalyst reached the highest yield of furan-2-acrolein (70%) after 3 h of reaction at 170 °C. This better catalytic performance can be explained by the high basicity of MgO, used as support, together with the large amount of available PdO, as inferred from XPS.