Showing papers in "European Journal of Chemistry in 2012"

Synthesis and antimicrobial activities of pyrido[2,3-d]pyrimidine, pyridotriazolopyrimidine, triazolopyrimidine, and pyrido[2,3-d:6,5d']dipyrimidine derivatives

Abstract: A new series of pyridotriazolopyrimidines were synthesized via reaction of hydrazonoyl halides with pyrido[2,3- d ]pyrimidines. The structures of the newly synthesized compounds were established by elemental analysis, spectral data and alternative synthetic routes whenever possible. Some of synthesized compounds were also screened in vitro for their antimicrobial activity against a variety of bacterial and fungal samples.

Development and validation of a reversed-phase column liquid chromatographic method for simultaneous determination of two novel gliptins in their binary mixtures with Metformin

Abstract: A new, simple, accurate, and precise liquid chromatographic method has been developed and validated for the determination of two novel dipeptidylpeptidase-4 (DPP-4) inhibitors; namely vildagliptin (VLG) and saxagliptin HCl (SXG) simultaneously in their binary mixtures with metformin HCl (MET). Chromatographic separation was achieved on an Inertsil® CN-3 column (250 mm x 4.6 mm, 5 µm). Isocratic elution using a mobile phase of potassium dihydrogen phosphate buffer pH (4.6) - acetonitrile (15:85, v:v) at a flow rate of 1 mL/min with UV detection at 208 nm was performed. The liquid chromatographic method was used for the simultaneous determination of either VLG, SXG and MET in the range of 5-200, 0.5-20 and 50-2000 μg/mL, respectively. The methods developed were satisfactorily applied to the analysis of the pharmaceutical formulations and proved to be specific and accurate for the quality control of the cited drugs in pharmaceutical dosage forms.

Recent progress in the asymmetric Mannich reaction

Abstract: The asymmetric Mannich reaction is one of the most useful carbon-carbon bond forming reactions for the synthesis of chiral molecules containing nitrogen. The resulting β-amino carbonyl compounds are valuable synthons in the preparation of many natural products with useful biological properties. In recent years, asymmetric Mannich processes have increasingly been reported and used in a rapidly growing number of applications. This review provides an overview of the recent history of the applications of various catalytic systems in asymmetric Mannich reaction, including metal-based asymmetric organocatalysis, asymmetric organocatalysis, other chiral catalysis and no chiral catalysis systems.

Photophysical properties and estimation of ground and excited state dipole moments of 7-diethylamino and 7-diethylamino-4-methyl coumarin dyes from absorption and emission spectra

Abstract: In the present work, the effect of solvents on absorption and fluorescence spectra and dipole moments ( μ g , μ e ) of 7-diethylamino coumarin (7DEAC) and 7-diethylamino-4-methyl coumarin (7DEA4MC) have been studied in different solvents of various polarity at room temperature. The solvents have been selected in a way to cover the full range of intermolecular interactions from non-polar hexane to strongly polar formamide. Using the methods of solvatochromism, the difference in the first excited singlet-state ( μ e ) and ground state ( μ g ) dipole moments was estimated from Lippert-Mataga, Bakhshiev, Kawski-Chamma-Viallet and McRae equations. The Onsager’s cavity radius of the probes has been calculated by AM1 and PM3 quantum chemical calculations and also by a direct relation. The change in dipole moment value (Δ μ ) was also calculated by using the variation of Stoke’s shift with microscopic solvent polarity parameter ( E T N ). The calculated dipole moments represent new results, as well as some of the solvatochromic results that were not studied earlier in such large number of solvents. It is observed that the values of excited singlet-state dipole moments are higher than the ground state ones in both the molecules, which shows that excited states are more polar than the ground states.

The chemistry of group-VIb metal carbonyls

Abstract: The special interest attached to the chemistry of metal carbonyls arises from several causes. While quite distinct from the metal carbonyls in the organometallic compounds, they differ in physical properties (e.g., their volatility) from all other compounds of the transition metals. Chemically, they constitute a group of compounds in which the formal valency of the metal atoms is zero, and in this respect (apart, perhaps, from the ammoniates of the alkali metals) they are comparable only with the recently discovered compounds. As a class, the carbonyls are reactive compounds, and a number of new types of inorganic compounds have been discovered. In the concepts for new products, performance, product safety, and product economy criteria are equally important. They are taken into account already when the raw material base for a new industrial product development is defined. Since the discovery of nickel carbonyl by Mond and Langer in 1888, the carbonyls of the iron group and of chromium, molybdenum and tungsten have found important technical applications, e.g., in the Mond nickel process, and for the preparation of the metals in a state of subdivision and of purity suitable for powder metallurgy, for catalysts, etc. The reaction mechanism of the processes developed for producing the carbonyls technically has only recently received its interpretations. Within the space of review it is necessary to limit discussion to a few topics. Particular stress has accordingly laid upon (a) the chemical bonding in metal carbonyls, (b) importance of IR and NMR spectroscopy in characterization of metal carbonyls, (c) substitution reactions of G-VIb metal carbonyls, (d) kinetics and mechanism of substitution reactions in metal carbonyls, (e) substituted complexes of G-VIb metal carbonyl, (f) chelate complexes of G-VIb metal carbonyls, (g) uses of G-VIb metal carbonyl complexes and (h) studies done on G-VIb metal carbonyls.

Knoevenagel condensation of isatins with malononitrile/ethyl cyanoacetate in the presence of sulfonic acid functionalized silica (SBA-Pr-SO3H) as a new nano-reactor

Abstract: The Knoevenagel condensation between isatins and active methylene compounds like malononitrile and ethyl cyanoacetate to prepare 2-oxoindolin-3-ylidene malononitrile/ cyanoacetates is described. The reactions occur in the presence of sulfonic acid functionalized silica SBA-15 (SBA-Pr-SO 3 H) in an aqueous medium giving excellent yields of the products in short reaction times. SBA-Pr-SO 3 H with a pore size of 6 nm is found to be an efficient and environmentally benign catalyst for this reaction.

Synthesis of bis(indolyl)methanes using molten N-butylpyridinium bromide

Abstract: A simple and rapid protocol has been developed for the synthesis of bis (indolyl)methane compounds in excellent yields using molten N -butyl-pyridinium bromide as a solvent and a working catalyst for the reaction. Synthesis of bis (indolyl)methane compounds were accomplished at moderate experimental conditions of temperature and ambient pressure, also involving an electrophilic substitution reaction of indoles with several aromatic aldehydes. The derivatives were confirmed with mass and other usual spectroscopic techniques. A discussion on plausible mechanism for the reaction is also presented.

Application of sulfonic acid functionalized nanoporous silica (SBA-Pr-SO3H) in the solvent free synthesis of (E)-arylidene-1,3-dihydroindole-2-ones

Abstract: An efficient and green condensation reaction is developed for the synthesis of ( E )-arylidene-1,3-dihydroindole-2-ones; (1), using heterogeneous nanoporous acid catalyst of SBA-Pr-SO 3 H with pore size, 6 nm in solvent free condition. Arylidene-1,3-dihydroindole-2-ones have many pharmaceutical properties such as Tyrosin kinase inhibiton. This method has the advantages of short reaction time, isolation ease of the products, excellent yields and recyclable catalyst.

Recyclable and reusable nano-CuFe2O4 catalyzed C-O cross-coupling

Abstract: An efficient protocol was developed and validated for the synthesis of biaryl/aryl alkyl ethers using CuFe 2 O 4 nano powder as a recyclable catalyst via the reaction between aryl halides and phenols/alcohols. Variety of aryl ethers were synthesized efficiently in the presence of catalytic amount of CuFe 2 O 4 , KOH as base, under ligand free conditions in nitrogen atmosphere with DMSO as solvent at 120 o C. The catalyst is air-stable, inexpensive, magnetically separable and recyclable up to four cycles.

Microwave-assisted solvent free efficient synthesis of 1,3,4-oxadiazole-2(3H)-thiones and their potent in vitro urease inhibition activity

Abstract: An efficient solvent free microwave assisted synthesis of 5-substituted-1,3,4-oxadiazole-2(3 H )-thiones (2a-2r) from hydrazides and carbon disulfide has been accomplished in good to excellent yield. The urease inhibition activity of the resulting compounds was investigated. Preliminary bioassay indicated that the compound 2j bearing 2-bromo substituent is the most active inhibitor exhibiting IC 50 12.60 ± 0.92 μ M.

Ziziphus mauritiana leaves extracts as corrosion inhibitor for mild steel in H2SO4 and HCl solutions

Abstract: The inhibition performance of extracts of Ziziphus mauritiana on mild steel corrosion in 0.5 M H 2 SO 4 and 0.5 M HCl was investigated using gravimetric, electrochemical polarization, electrochemical impedance spectroscopy and scanning electron microscopic studies. The gravimetric results indicate that Ziziphus mauritiana leaves extract exhibits good inhibition efficiency in both the acids. Furthermore, the inhibition efficiency decreases with increase in temperature. Polarization measurements showed that the studied inhibitor is mixed type in both acids with significant reduction of cathodic and anodic current densities. Electrochemical impedance spectroscopy measurements revealed that the charge transfer resistance increases with increase in the concentration of Ziziphus mauritiana extracts. Various thermodynamic parameters such as activation energy, activation enthalpy and activation entropy are evaluated and discussed. Adsorption thermodynamic parameters are also computed, and SEM was used to analyze the surface adsorbed film.

Photocatalytic degradation of methylene blue using a zinc oxide-cerium oxide catalyst

Abstract: The photocatalytic degradation of methylene blue in aqueous solution was studied using a UV source in the presence of zinc oxide-cerium oxide (ZnO-Ce 2 O 3 ) as photocatalyst, which was synthesized by a gel combustion technique and characterized by X-ray diffraction, scanning electron microscopy, and energy dispersive X-ray spectroscopy. The particle size of the catalyst was found to be in between 45 to 60 nm. The effects of catalyst loading (1.0-8.0 g/L), pH (4.0-9.2) and dye concentration (5.0-20.0 mg/L) on the degradation were studied in a batch reactor. The degradation rate was found to be strongly dependent on these experimental parameters. Appreciable degradation of methylene blue was achieved when the catalyst was calcined before use. Best results were observed with a catalyst loading of 5 g/L at pH = 9.2.

Simultaneous determination of miconazole and hydrocortisone or mometasone using reversed phase liquid chromatography

Abstract: Two simple, rapid and precise reversed phase liquid chromatographic methods have been developed and validated for the simultaneous determination of miconazole nitrate in two binary mixtures, with hydrocortisone acetate (Mixture 1) and mometasone furoate (Mixture 2). For the two mixtures, chromatographic separation was carried out on a C18 column. For mixture 1, a mobile phase consisting of 2.22 mM sodium dihydrogen phosphate (Triethylamine 0.2%):acetonitrile (45:55, v : v ) at a flow rate of 0.9 mL/min was used at ambient temperature. Quantitative determination of miconazole and hydrocortisone was achieved with UV detection at 215 and 245 nm, respectively. Linearity, accuracy and precision were found to be acceptable over the concentration range of 30-80 μg/mL for miconazole and 4-80 μg/mL for hydrocotisone. For mixture 2, a mobile phase consisting of acetonitrile:water (Triethylamine 0.2%) (70:30, v : v ) at a flow rate of 0.9 mL/min was used at ambient temperature. Quantitative determinations of miconazole and mometasone were achieved with UV detection at 215 and 250 nm, respectively. Linearity, accuracy and precision were found to be acceptable over the concentration range of 10-200 μg/mL for miconazole and 2-60 μg/mL for mometasone. The optimized methods were proved to be specific, robust and accurate for the quality control of the cited drugs in pharmaceutical preparations.

Solvent effect on the spectral properties of dipolar laser dyes: Evaluation of ground and excited state dipole moments

Abstract: The effect of solvents on absorption and fluorescence spectra and dipole moments of two medium sized dipolar laser dyes 2-(2,7-dichloro-6-hydroxy-3-oxo-3 H -xanthen-9-yl) benzoic acid (Fluorescein 27) (F27) and N -[6-diethylamino)-9-(2,4-disulfophenyl)-3 H -xanthen-3-ylidene]- N -ethylhydroxid (Sulfarhodamine B) (SRB) have been studied comprehensively in polar protic and polar aprotic solvents at room temperature (298 K). The bathochromic shift observed in absorption and fluorescence spectra of F27 and SRB with increasing solvent polarity signifies that the transition involved are π→π*. Solvatochromic correlations were used to obtain the ground and excited state dipole moments. The observed excited state dipole moments are found to be larger than their ground state counterparts in all the solvents studied. The ground and excited state dipole moments of these probes have also been computed from ab initio calculations and compared with those determined experimentally. Further, the experimentally obtained changes in dipole moment (Δ μ ) were compared with those using normalized polarity terms from Reichardt equation.

Synthesis of an E-BODIPY based fluorescent Co-polymer containing organoboron quinolate units

Abstract: A novel fluorescent co-polymer with an organoboron quinolate and an E -BODIPY (BODIPY: 4,4-difluoro-4-bora-3a-4a-diaza- s -indacene) moiety was synthesized with the aim of producing a donor-acceptor polymeric system where the organoboron quinolate acts as the donor and the E -BODIPY moiety is the acceptor. The polymer has three prominent absorption bands: 264 nm (corresponding to the organoboron quinolate), 397 nm (corresponding to the organoboron quinolate and BODIPY) and 516 nm (corresponding to the E -BODIPY moiety). Excitation of the organoboron quinolate at 264 nm resulted in emission at 525 nm, giving a 261 nm Stokes shift. Energy transfer from the donor (organoboron quinolate) unit to the acceptor (BODIPY) explains the origin of this large Stokes shift.

Reactivity of β-enamino ester of benzo[f]chromene: One pot synthesis of isolated and heterocycle-fused derivatives of benzo[f] chromene

Abstract: The formation of isolated and fused benzo[ f ]chromene derivatives was achieved via reacting ethyl 3-amino-1-phenyl-1 H -benzo[ f ]chromene-2-carboxylate ( 1 ) with some selected reagents under basic conditions. The new compound, ethyl 3-(dimethylaminomethyleneamino)-1-phenyl-1 H -benzo[ f ]chromene-2-carboxylate ( 2 ) was prepared from compound 1 and N , N -dimethyl formamide in presence of phosphorus oxychloride under mild conditions in excellent yield using Vilsmeier reaction. Also, 10-amino-12-phenyl-9-sulfanyl-12 H -benzo[ f ] chromeno[2,3- d ]pyrimidine-11(10 H )-one ( 12 ), 10-aryl-14-phenyl-14 H -benzo[ f ]chromeno [2,3- d ][1,3,4]thiadiazolo[3,2- a ]pyrimidine-13-one ( 15 ), ethyl 3-(4-oxo-2-thioxothiazolidin-3-yl)-1-phenyl-1 H -benzo[ f ]chromene-2-carboxylate ( 18 ), ethyl 3-(4-phenyl-2-thioxothiazol-3(2 H )-yl)-1-phenyl-1 H -benzo[ f ]chromene-2-carboxylate ( 20 ), ethyl 3-acetamido-1-phenyl-1 H -benzo[ f ]chromene-2-carboxylate ( 21 ), and 10-amino-9-methyl-12-phenyl-12 H -benzo[ f ] chromeno[2,3- d ]pyrimidine-11(10 H )-one ( 23 ) were prepared . The structures of these compounds were established by elemental analysis, IR, MS and NMR spectral analy­sis.

Convenient synthesis of some new pyrazolo[5,1-c]triazines, isoxazolo[3,4-d] pyrimidine and pyridine derivatives containing benzofuran moiety

Abstract: Pyrazolo[5,1- c ][1,2,4]triazine, [1,2,4]triazolo[3,4- c ][1,2,4]triazine, benzo[4,5]-imidazo[2,1- c ][1,2,4]triazine, isoxazole, isoxazolo[3,4- d ]pyridazine, pyrazole, pyridine, substituted urea and phenyl carbamate derivatives containing benzofuran moiety were synthesized via reaction of sodium salt of 5-hydroxy-l-benzofuran-2-ylpropenone or 1-(benzofuran-2-yl)-3-(dimethylamino)prop-2-en-1-one with diazotized heterocyclic amines, hydroximoyl chlorides and active methylene compounds. The structures of all the newly synthesized compounds were confirmed by elemental analyses, spectral data, and alternative synthetic routes, whenever possible.

Synthesis, spectral characterization and biological evaluation of 4H-1,4-benzothiazines, their sulfones and ribofuranosides

Abstract: Synthesis of heterocyclic compounds like benzothiazines has attracted attention in recent years due to their biological and industrial value. This article reflects up-to-date and comprehensive coverage of biochemical aspects of benzothiazines, their sulfones and ribofuranosides. The nitrogen and sulfur containing heterocycles were prepared by condensation followed by oxidative cyclization of 2-aminobenzenethiol with β-diketones/β-ketoesters in dimethylsulfoxide. These compounds were then used as base to prepare ribofuranosides by treating them with sugar (β-D-ribofuranose-1-acetate-2,3,5-tribenzoate). On refluxing with hydrogen peroxide in glacial acetic acid, these substituted dimethyl 4 H -1,4-benzothiazines yielded 4 H -1,4-benzothiazine-1,1-dioxides. Antioxidant and antimicrobial activity of these compounds were carried out and structure evaluation was done by spectral and elemental analysis.

Application of SBA-Pr-SO3H in the synthesis of benzoxazole derivatives

Abstract: Propylsulfonic acid functionalized SBA-15 (SBA-Pr-SO 3 H) catalyzed the synthesis of 2-aryl benzoxazoles from 2-aminophenol and benzoyl chloride derivatives in good yields under reflux condition in acetic acid. In solvent free condition, hydroxybenzanilide derivatives were obtained.

Studies towards the synthesis of (±)-reserpine: Photocyclization mediated a novel and efficient synthesis of 11,18-dimethoxy-(20α)-18,19-didehydro-yohimban-17-one

Abstract: A short, highly efficient synthesis of advanced intermediates to reserpine 1 has been developed starting from enamide 8 . The enamide underwent photocyclization reaction using high pressure mercury lamp to afford the lactam 9 in excellent yield. Then lactam was reduced to the required amine 10 , which upon acidic hydrolysis gave the nonconjugate ketone product 11 , followed by reaction with sodium hydroxide resulted the desired conjugate ketone 12 . Epoxidation, and then ring opening of the epoxide 13 with methanol yielded the desired product 14 , which is key intermediate to the total synthesis of (±)-reserpine.

Conductometric titration method for determination of naftidrofuryl oxalate, propafenone HCl and sotalol HCl using silver nitrate

Abstract: A simple, precise, rapid, and low-cost conductometric method for determination of naftidrofuryl oxalate, propafenone HCl and sotalol HCl in pure form and in pharmaceutical formulations using silver nitrate has been described. The method is based on the precipitation of oxalate or chloride ions coming from the cited drugs with silver ions, yielding silver oxalate or silver chloride and the conductance of the solution is measured as a function of the volume of titrant. The studied drugs were evaluated in double distilled water in the range of 1-15 mg. Various experimental conditions were established and results obtained showed good recoveries with relative standard deviation of 0.909, 0.955 and 0.983 for naftidrofuryl, propafenone and sotalol, respectively. The proposed procedures were applied successfully to the analysis of these drugs in their pharmaceutical formulations. Results were favorably comparable to the official or reference methods.

Determination of excited singlet-state dipole moments of hydroxy and methoxy coumarins using solvatochromic method

Abstract: The effects of solvents of various polarity on the electronic absorption and fluorescence spectra of 7-hydroxy-4-trifluoromethyl coumarin; 6,7-dihydroxy-4-trifluoromethyl coumarin and 7-methoxy-4-trifluoromethyl coumarin have been investigated. The singlet-state excited dipole moments ( μ e ) and ground state dipole moments ( μ g ) are estimated from Bakshiev and Kawski-Chamma-Viallet equations by using the variation of Stokes’ shift with the solvent’s dielectric constant ( e ) and refractive index ( n ). The observed singlet-state excited dipole moments are found to be larger than the ground-state ones. In addition, the geometry and other electronic properties are computed using ab-initio method with correlation functions at 6-31G basis set.

Crystal and molecular structure of bis(4-bromo-N-(di-n-butylcarbamothioyl)benzamido) copper(II) complex

Abstract: The title compound, C 32 H 44 Br 2 CuN 4 O 2 S 2 , was synthesized from 4-bromo- N -(dibutylcarbamothioyl)benzamide ligand and copper(II)acetate. The crystal structure of bis (4-bromo- N -(di- n -butylcarbamothioyl)benzamido) copper(II) complex was determined from single crystal X-ray diffraction studies. It crystallizes in the triclinic space group, P -1 (no. 2) with unit cell dimensions of a = 8.519(10) A, b = 16.64(2) A, c = 25.78(4) A, α = 77.11(3) o , β = 85.59(3) o , γ = 89.46(2) o , Z = 4 and V = 795.8(6) A 3 . The crystal structure is stabilized by weak C-H…N, C-H…S and C-H…Br hydrogen-bonding interactions.

Calix[4]pyrrole macrocycle: Extraction of fluoride anions from aqueous media

Abstract: Solid-phase extraction of fluoride anions by calixpyrrole macrocycle (CP) from aqueous media has been studied using the batch method. Various significant extraction parameters like initial concentration of the anion, extraction time, concentration of the calixpyrrole, pH and temperature were evaluated. Langmuir, Freundlichand, Dubinin-Redushkevish (D-R) isotherms and coefficients were used to analyze the equilibrium data. The amount of fluoride anion extracted per unit of the CP was found to be 0.40 mg/g at 298 K from 19 mg/L aqueous solution of fluoride anions. The mean free energy calculated from D-R model for the removal of fluoride anions by the CP was found to be 10.0 kJ/mol, indicating that chemisorption is involved in the extraction process. The data were also fitted to kinetic models such as pseudo first order and pseudo second order. The removal of fluoride anions increased with increasing temperature indicating the endothermic nature of the extraction process. The present method has been compared with the previous methods.

Anticancer activity studies of some cyclic benzimidazole derivatives

Abstract: New benzimidazole derivatives, namely, ( N -(4-methoxyphenyl)methylene]-1H-benzimidazol-2-amine (2a), ( N -(3,4-dimethoxyphenyl)methylene]-1 H -benzimidazol-2-amine (2b), and ( N -(3,4,5-trimethoxyphenyl)methylene]-1 H -benzimidazol-2-amine (2c) were synthesized by reaction of a Schiff base with malononitrile in absolute ethanol. Structures of compounds have been confirmed by IR, 1 H NMR and elemental analysis. Compounds 2a-c were screened for their in vitro anticancer potential using HeLa and PC3 cells. All compounds showed limited cytotoxicity except compound 2a that showed a moderate cytotoxic effect towards HeLa cells.

Efficient deprotection of Boc group in amines and sulfamides using Dawson heteropolyacid catalyst

Abstract: A series of sulfamides containing two protecting groups have been synthesized starting from N -benzoylaminoacids derivatives of (glycine, alanine, valine, leucine, phenylalanine), chlorosulfonylisocyanate and primary amines. Selective deprotection of the cyclic or linear sulfamides and amines has been achieved by treatment with heteropolyacid, which is easily recoverable and reusable. This method represents a reasonable alternative to the previous reported deprotection procedures.

Potassium hydrogen sulfate: An efficient catalyst in organic reactions

Abstract: Potassium hydrogen sulfate, KHSO 4 , has been used in many organic preparations as a good solid catalyst. The KHSO 4 has received considerable attention since it is an inexpensive, eco-friendly, highly reactive, easy to handle and non-toxic catalyst for various organic transformations, affording the corresponding products in excellent yields with high selectivity. We wish to report some applications of this catalyst in organic reactions.

Synthesis of ethylene carbonate from cyclocondensation of ethylene glycol and urea over ZnO•Cr2O3 catalyst system controlled by co-precipitation method

Abstract: ZnO·Cr 2 O 3 catalyst has been synthesized by low temperature, pH controlled co-precipitation route and characterized employing techniques of Brunauer, Emmett, and Teller (BET) surface area measurement, ammonia desorption technique, X-ray diffraction (XRD) and scanning electron microscopy (SEM). These characterizations reveal the catalyst to possess ZnO·ZnCr 2 O 4 composition. The catalysts have been tested for their performance for the first time, in the synthesis of ethylene carbonate from cyclocondensation of ethylene glycol and urea. Effect of catalyst concentration, temperature and molar ratio of reactants has been studied to obtain the optimum conversion and selectivity of ethylene glycol and urea to ethylene carbonate. A maximum yield of 85.75% of ethylene carbonate was obtained at a temperature of 423 K and urea: ethylene glycol molar ratio of 1:1.5. A tentative mechanism of the reaction is proposed on the basis of analysis of reactants, products and modeling of the transition state for the reaction under density function theory using Gaussian09W software. Our studies suggest a consecutive mechanism for the reaction. In the first step, urea and ethylene glycol react to produce 2-hydroxyethyl carbamate, which undergoes further reaction to produce ethylene carbonate (EC) and ammonia.

Synthesis of novel 2-propenoyl amides, esters, heterocyclic compounds and their screening as antifungal and antibacterial agents

Abstract: Compound, 2-cyano-3-(2 ˊ ,4ˊ-dichlorophenyl)-2-prpoenoyl chloride, 3 , was reacted with nitrogen, sulfur, and oxygen nucleophilic reagents to give new 2-propenoyl amide and ester derivatives. Some of these derivatives were cyclized under the reaction conditions and/or with POCl 3 or Ac 2 O to give new derivatives of heterocyclic systems. Some of these compounds were tested as antibacterial and antifungal agents.

In-vitro cytotoxic and radiosensitizing evaluation of novel 2-pyridone, isoquinoline, chromene and chromenopyridone derivatives

Abstract: On the account of the reported anticancer activity of 2-pyridone, a new series of ethyl-1,6-dihydropyridine-3-carboxylate ( 4a - j ), 1-oxo-1,2-dihydroisoquinoline-7-carbonitrile ( 6a - h ), 2 H -chromene ( 7 , 8 ) and 3 H -chromeno[3,4- c ]pyridone derivatives ( 9 , 10 ) were synthesized and tested for in-vitro anticancer activity against Ehrlich Ascites Carcinoma (EAC) cell line and human liver cell line (HEPG2). The structures of the synthesized compounds were confirmed by analytical and spectral data. Furthermore, radiosensitization study was performed for the most potent compounds ( 4a , 4d , 6a , 6c , 6e and 10 ).