Background: A ligand free, microwave assisted, copper catalyzed synthetic procedure for substituted tertiary amines has been developed by using nitroarenes and secondary amines. Methods: In the synthetic method, the targeted substituted tertiary amines were synthesized with the help of the microwave by reacting nitroarenes and substituted secondary amines in the presence of copper, potassium carbonate and methanol. Results: All substituted tertiary amines were obtained in good yields (88-94%) with the help of a microwave technique (07-12 min) in less time. The protocol adopted was ligand free. Conclusion: Microwave assisted technique will be a useful alternative protocol for the preparation of a diverse range of substituted tertiary amines.

Background: An efficient, microwave assisted, copper catalyzed synthetic protocol for substituted benzamides has been developed by using salts of carboxylic acids. Methods: In the synthetic method, the targeted substituted benzamides were synthesized with the help of microwave by reacting salts of carboxylic acid and benzamides in the presence of copper and dimethyl formamide. Results: All substituted benzamides were obtained in good yield (93-99%) with the help of a microwave technique (12-15 min) in the less time as compared to the conventional method. Conclusion: Microwave assisted technique will be a useful alternative protocol for the preparation of diverse range of substituted benzamides.

A series of novel molecules containing thiazole ring structure were designed and synthesized. The structures of the synthesized compounds were elucidated and confirmed by (1)H NMR, (13)C NMR, Mass spectrum and the purity was checked through HPLC analysis. Among these synthesized compounds, 3a-3i and 6a-6c were tested for their antimicrobial activity (minimum inhibitory concentration) against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus niger for antifungal activity respectively. The results of the antimicrobial screening data revealed that most of the tested compounds showed moderate to good microbial inhibitions.

Background: Although several methods are reported for the C-S bond formation, the microwave assisted method reported in this work is simple and proceeds with high yields in short time.Methods: In the synthetic method, the targeted aryl sulfides were synthesized with the help of microwave by reacting halobenzenes, substituted thiophenols and potassium carbonate in the presence of dimethyl sulfoxide and water.Results: All the aryl sulfides were obtained in good yield (87%-97%) with the help of microwave technique and in the presence of dimethyl sulfoxide: water as a solvent system.Conclusion: Microwave assisted synthesis will be a useful alternative method for the synthesis of diverse range of aryl sulfides.

Objective: The objective of the present study was to develop potent and non toxic Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) by using heterocyclic nuclei and having Nitric Oxide releasing group. Methods: The compounds were designed with the help of docking studies. In the synthetic study, the target compounds were obtained by reacting substituted diphenyl imidazole benzoic acid (2a-2x) with nitro-oxy alkyl bromide in the presence of dimethyl formamide and potassium carbonate to give substituted 2,4-diphenyl nitric oxide releasing imidazole derivatives (3a-3x). The synthesized compounds were characterized with the help of different analytical studies and further evaluated for anti-inflammatory, analgesic and nitric oxide releasing activity. Results: In the docking study compounds 3a, 3b, 3c, 3e, 3r and 3s showed significant G-score. In the anti-inflammatory and analgesic study compounds 3a, 3b, 3c, 3e, 3r and 3s exhibited promising activity. All the synthesized compounds exhibited significant nitric oxide releasing properties both in-vitro and in-vivo . Conclusion: Compounds 3a, 3b, 3c, 3e, 3r and 3s exhibited prominent anti-inflammatory and analgesic activity.

A series of semi-rigid N-phenylsuccinimides I (11Xy), N-arylmethylsuccinimides II (18Xy), and N,N′-(1,4-arylenebis(methylene))disuccinimides III (19XyX) walled by quinoxaline (QX), dimethylquinoxaline (diMQX), or benzoquinoxaline (BQX) ring were synthesized. Intramolecular π–π interactions in solution were detected by NMR and fluorescence spectroscopy, in terms of reciprocal anisotropic shielding and exciplex formation, respectively. The X-ray crystallographic analysis revealed the preferential conformations in solid state, which were compatible with the results of conformational studies by NMR and fluorescence spectroscopy. The results collectively indicated that 18Xy and 19XyX are driven by intramolecular π–π interactions in the mode of π-stacking (face-to-face) or T-shaped (edge-to-face) configuration to preferentially adopt the folded- and the double folded-conformation, respectively, where the spaced aromatic rings are oriented syn to each other in close proximity.

An efficient, microwave-assisted ligand-free, catalyst-free synthetic method for nonsymmetrical diaryl ethers has been developed by using nitroarenes. A variety of phenols and nitroarenes was scanned by using this method to produce nonsymmetrical aryl ethers. The newly developed method is an ecofriendly and cost-effective approach to synthesize nonsymmetrical aryl ethers.

An efficient, CuI catalyzed, ligand free, synthetic protocol for thioethers has been developed by using nitroarenes. A variety of thiols and nitroarenes was scanned by using this method to produce aryl sulfides. Newly developed method demonstrates a new alternative to existing method which is cost effective approach to synthesize nonsymmetrical aryl thioethers.

The title compound 30 was synthesized starting from the endo,syn,endo Diels-Alder adduct 3a of hexahydro-5,6,7,8-tetrachloro-9,9-dimethoxy-5,8-methanonaphthalene-1,4-diol diacetate 6 and 1,2,3,4-tetrachloro-5,5-dimethoxycyclopentadiene (TDCp) in six steps, keyed upon a symmetry-allowed [4+4] photocyclization of decahydro-11, 12-dioxo-[1,4;5,8]dimethanoanthracene-9,10-diol diacetate 22. The epimeric monoacetate 26 related to 22 was also synthesized and their thermolysis and photolysis were investigated. Oxidation of diol 30 afforded hexacyclic bridged hemiacetal 31 as a result of transannular reaction. The structure of hemiacetal 31 was analyzed by single-crystal X-ray crystallography.

Chlorosulfonic acid is used as an alternative to conventional acid catalysts in the von Pechmann condensation of phenol with β-ketoester leading to the formation of substituted coumarin.

AbstractFor Abstract see ChemInform Abstract in Full Text.

The substituted 3,4-dihydropyrimidin-2(1H)-ones and their thione analogues have been prepared Via Biginelli condensation using aldehyde, 1,3-dicarbonyl compound and urea or thiourea under the catalyst of sulphamic acid (H2NSO3H). The method is simple, cost-effective, and gives good yields in a shorter reaction time.

The synthesis, characterization and anti-inflammatory activity of dipyrazolopyridine derivatives are described.

Samarium(III) nitrate hexahydrate as a catalyst is used as an alternative to conventional acid catalysts in the von Pechmann condensation of phenols with ethyl acetoacetate leading to the formation of coumarin derivatives.

The use of the ionic liquid [bmim]Cl.2AlCl3 for the preparation of dihydropyrimidinones is described.

A series of [4,6-(substituted aryl)-2-thioxo-1,2,3,4-tetrahydro-pyrimidin-5-yl]-acetic acid (4a-r) has been synthesized by the base catalyzed condensation of beta-aroylpropionic acid, thiourea with aldehyde in ethanol. Structures of the new compound were established on the basis of (1)H NMR and IR spectral data. Anti-inflammatory activity in vivo were evaluated and compared with standard drug diclofenac sodium. Some compounds have shown moderate activity.

Dihydropyrimidines 4a-r have been synthesized by base catalysed condensation of beta-aroylpropanoic acid, guanidine nitrate and aromatic aldehyde. Structures of the new compounds were established on the basis of 1H NMR and IR spectral data. Anti-inflammatory activity in vivo was evaluated and compared with standard drug diclofenac sodium.

소염작용을 가진 일련의 싸이아졸리딘아세트산 유도체들을 싸이오유레아와 말레산무수물로부터 합성하고 분광학적인 방법으로 구조를 확립하였다. 또한 이 화합물들의 소염작용을 표준시약인 디클로펜악 소듐과 비교한 결과 어느정도의 효과를 가지고 있음을 검정하였다. A synthetic method for the title compounds (2a-o) was carried out. The title compounds (2a-o)were prepared by the condensation of various thioureas and maleic anhydride. Anti-inflammatory activities in vivo were evaluated and compared with standard drug diclofenac sodium. Some compounds showed moderate activity. The structures of all the new compounds were established on the basis of $^1H$ NMR and IR spectral data.

일련의 옥사졸론 유도체들을 (4a-n) 항균제로서 합성하였다. 이 화합물들은 아릴옥시아세틸아미노아세트산을 에탄올, 아세트산 무수물, 아세트산 소듐 존재하에 알데하이드와 반응시켜 합성하였으며 핵자기공명 스펙트럼과 적외선 스펙트럼으로 구조를 확인하였다. A series of oxazolone derivatives (4a-n) have been synthesized as a potential antibacterial agent. Titled compounds have been prepared by the condensation of aryloxy acetyl-amino-acetic acid with aldehyde in presence of ethanol, acetic anhydride and sodium acetate. The structures of the new compounds were established on the basis of $^1H$ NMR and IR spectral data.