4a-Methyl-2,3,3,4a-tetrahydro-1H-carbazoles 3, obtained from arylhydrazines 1 and 2-methylcyclohexanone 2, react with diethyl malonate 5a by cyclocondensation to 7-hydroxy-13b-methyl-tetrahydro-pyrano[2',3':4,5]pyrido[3,2,1-jk]carbazolediones 6. With methanetricarboxylates 5b,c, cyclocondensation forms a mixture of pyrano-pyrido-carbazole-carboxylates 7 and pyrido-carbazole-carboxylates 8. Degradation of pyrano-pyrido-carbazolediones 6 by alkaline ring-opening and decarboxylation leads to 5-acetyl derivatives 10. Deacetylation with sulfuric acid reveals the 5-unsubstituted 4-hydroxy-11b-methyl-1,2,3,11b-tetrahydro-6H-pyrido[3,2,1-jk]carbazol-6-one (9). Pyridocarbazolone 9 was also obtained in a single step reaction from tetrahydrocarbazole 3a and malonic acid 5d with phosphoryl chloride as catalyst in low yields.
Electrophilic halogenation of 9 takes place at position 5 and gives 5-bromo compound 15 or 5,5-dihalogenated products 14, 16 or 17, depending on the reaction conditions. Nitration takes also place in an electrophilic reaction to give 4-hydroxy-5-nitro-pyrido-carbazolone 20. Nucleophilic exchange of the 4-hydroxy group in pyridocarbazolones 9 and 20 by reaction with phosphoryl chloride gives reactive 4-chloro intermediates 18 and 21, which react with sodium azide to 4-azido derivatives 19 and 22. 4-Azido-5-nitro-pyrido-carbazolone 22 with the reactive ortho-nitro group in the neighborship of the azido group cyclizes thermolytically to furoxane 23. This reaction was studied by differential scanning calorimetry (DSC).

The benzofuran scaffold is ubiquitous in the area of pharmacologically active agents and isolated natural products. Natural products possessing the 2-substituted moiety exhibit a broad range of pharmacological activities such as antimicrobial, anti-inflammatory, antifungal, antipsychotic, antilipidemic, analgesic, cytotoxic and central nervous system stimulant. Also, benzofuran nucleus has been recently described as a good scaffold for designing potent and relatively non-selective MAOIs.

The synthesis and identification of novel 2-eteroarylbenzofuran derivatives with electron-donating and electron-withdrawing substituents are reported in this work.

The key step for the formation of the benzofuran moiety was achieved by an intramolecular Wittig reaction between ortho-hydroxybenzyltriphosphonium salts and the appropriate aroyl chlorides.

Their complete structural characterization was performed using one-dimensional and two- dimensional resonance techniques. The acquired data constitute a valuable database for the unambiguous identification of eteroarylbenzofuran library developed with the aim of our medicinal chemistry program.

This communication reports the synthesis of a series of new (-)menthylalkyltin dihydrides of type (-)MenRSnH2 (R = Me, i-Pr, n-Bu, and t-Bu), starting from the known (-)MenMe2SnBr (1). These organotin dihydrides containing a bulky chiral (-)menthyl substituent and alkyl groups of increasing steric volume should be of interest in the reduction of prochiral ketones and unsaturated systems. Physical characteristics of the new diorganotin hydrides and some of their precursors including selected values1H, 13C, and 119Sn NMR data are given.

The reactivity of (E)-5-(4-hydroxy-3-methoxyphenyl)-1-phenylpent-4-ene-1,3-dione with ethylenediamine has been studied in different experimental conditions. Two dihydro-1,4-diazepines have been obtained and fully characterized by 1D and 2D multinuclear NMR spectroscopy and HRMS.

Abstract

An improved method for synthesis of 2,4-diacetyl-cyclohexanone derivatives is reported with enhanced yield in presence of DMSO as solvent. In situ, reaction of aromatic and hetero aromatic aldehydes with β-oxo-ketones undergoing Knoevenagel condensation, Michael addition followed by aldol condensation to give the desired product in excellent yield. displayed prominent mild to moderate antimicrobial and antifungal activities. The 2,4-diacetyl-cyclohexanone derivatives thus obtained have been characterized by ¹H NMR, ¹³CNMR, FT-IR, MASS, HRMS and X-ray single Crystallography  spectroscopic methods.

Recently, nickel ferrite has attracted attention due to its multiple applications in storage devices, microwave devices, gas sensors, ferrofluids and catalysts. Nickel ferrites have excellent optical properties owing to their small band gap, which makes them suitable as a photocatalyst.

Among methods to synthesize nanocrystalline NiFe₂O₄, combustion method seems to be one of the facile and one step methods, since it allows the preparation of nanocrystalline NiFe₂O₄ with an equiaxial shape and narrow size distribution. Applying surfactants, which are composed from molecules along with sol–gel method can improve the properties of the synthesized powders.

In this present study, the sol–gel auto-combustion method is applied for synthesizing the NiFe₂O₄/CTAB and NiFe₂O₄/SDS nanocomposite, using nickel nitrate, iron nitrate, ammonia, citric acid and CTAB and SDS as surfactant. The nanoparticles were characterized by XRD, SEM, FT-IR and DRS. Powder XRD analysis and FT-IR spectroscopy confirmed formation of NiFe₂O₄ spinel phase. The particles size was estimated from SEM data. The energy band gaps were calculated by Kubelk-Munk model from UV–Vis absorption.

Metal organic frameworks (MOFs) contain inorganic and organic networks that can be easily functionalized to get tuneable properties. MOFs as highly porous crystalline materials constructed by coordination bonds between metal ions/clusters and organic ligands, have developed very fast due to not only their intriguing structures but also the potential applications, such as gas separation, storage, and sensing. They have great potential as adsorbents/catalysts due to their extremely large surface area, well-ordered porous structures, and diverse means available for functionalization. MOF-5 consists of four [Zn₄O]⁶⁺ clusters in octahedral subunits that are connected to each other by terephthalate or benzene-1,4-dicarboxylate (BDC) groups, to form a porous cubic framework [3]. In this work, we have synthesized Ni-doped, MOF-5 by solvothermal method according to the literature. The Ni-MOF was formed with cubic structure but changing the reaction conditions resulted to the novel hexagonnal structure. The characterization was performed by FTIR, XRD and SEM methods.

Here is the report of an environment friendly, rapid, and convenient one-pot ultrasound-promoted synthesis of 5-amino-2-(4-chlorophenyl)-7- substituted phenyl-8,8a-dihydro-7H-[1,3,4]thiadiazolo[3,2-a]pyrimidine-6-carbonitrile derivatives. Multi-component reactions are useful for the creation of chemical libraries of drug-like compounds with levels of molecular complexity and diversity. 1,3,4-Thiadiazolo[3,2-a]pyrimidine skeleton belongs to a well-known and important class of fused heterocycles prevalent in a number of natural products of biological activities including antitumor, fungicidal, antibacterial, and herbicidal, hence, prompted us to synthesis 1,3,4-Thiadiazolo[3,2-a]pyrimidines. The final ten derivatives were obtained in excellent yield through a one-pot, three component condensation reaction of aldehyde, 4-chlorophenyl-2-aminothiadiazole, and malononitrile in 10-12 ml of ethanol as solvent and sodium hydroxide as a catalyst. (VCX 500-220, Ultrasound Solid probe, irradiation at 80⁰C and 20% amplitude).

We have carried out the same reaction by conventional method, which requires 9-10 hrs of refluxing and yield is lesser. Because of the advantage of faster reaction rates and better yields, use of Ultrasound solid probe, was found to be more suitable for this reaction. Structure of the synthesized derivatives was confirmed by IR, NMR and Mass spectral study.

Antimicrobial activity of different extracts of bark of Moringa oleifera was studied against ten bacterial strains These bacteria are both gram +ve and gram -ve. Bark were extracted with a petroleum ether, chloroform, ethyl acetate, ethanol and aqueous . In the present work the antibacterial activity was done by cup plate method. The antibacterial activity was expressed as zone diameter in millimeters. Different extracts from bark of the plant was compared with standards like benzyl penicillin for gram +ve bacteria and streptomycin for gram –ve bacteria using DMF as control. The readymade media for inoculum and culture was obtained from Himedia labs. Prepared herbal extracts from the bark of the plant were screened against bacteria organisms at the concentration range between 50 µg and 300 µg/0.1ml. The present investigation reveals that the aqueous, chloroform and ethyl acetate extracts and in some cases petroleum ether extract showed significant antimicrobial activity when compared with standard.

In the current paper we studied the interest of a series of 3-arylcoumarin derivatives as xanthine oxidase inhibitors. For the best compound of the series, the 4’-methoxyphenyl-6-nitrocoumarin, it was determined the IC₅₀ value and the type of inhibition. This work is a preliminary screening for further design and synthetize new non-purinergic derivatives as potential compounds involved in the inflammatory suppression, specially related to the gout.